m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03400
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[1], [2] | |||
Histone modification
H3K4me1
Epigenetic Regulator
MIR570HG
Indirect
Inhibition
m6A modification
MTOR
MTOR
METTL3
Methylation
: m6A sites
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| m6A Modification: | |||||
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| m6A Regulator | Methyltransferase-like 3 (METTL3) | WRITER | |||
| m6A Target | Serine/threonine-protein kinase mTOR (MTOR) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Regulated Target | Histone H3 lysine 4 monomethylation (H3K4me1) | View Details | |||
| Downstream Gene | MIR570HG | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Inhibition | |||
| Crosstalk Mechanism | Histone modification indirectly regulates m6A modification through downstream signaling pathways | ||||
| Crosstalk Summary | Gain of Histone H3 lysine 4 monomethylation (H3K4me1) and H3K27ac led to the activation of MIR570HG expression. LINC00969 interacts with EZH2 and METTL3, transcriptionally regulates the level of H3K27me3 in the NLRP3 promoter region, and posttranscriptionally modifies the m6A level of NLRP3 in an m6A-YTHDF2-dependent manner METTL3-mediated m6A methylation promotes lung cancer progression via activating PI3K/AKT/Serine/threonine-protein kinase mTOR (MTOR) pathway. | ||||
| Responsed Disease | Lung cancer | ICD-11: 2C25 | |||
| Responsed Drug | Gefitinib | ||||
| Cell Process | Pyroptosis | ||||
In-vitro Model |
A-549 | Lung adenocarcinoma | Homo sapiens | CVCL_0023 | |
| In-vivo Model | 5 × 106 A549 cells overexpressing METTL3 (Lv-METTL3) or control (Lv-Ctrl) were suspended in 100 uL phosphate-buffered saline (PBS), and were subcutaneously injected into mouse lower right flank. Drug treatment started in the Lv-METTL3 group when the tumour volume reached around 100 mm3. Mice were randomly divided into three groups to receive vehicle, GSK2536771 (30 mg/kg) or rapamycin (1 mg/kg). Drugs were administrated daily through intraperitoneal injection for 18 days. Treatment conditions were chosen as previously reported. | ||||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Serine/threonine-protein kinase mTOR (MTOR) | 72 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Novolimus | Approved | [3] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Temsirolimus | Approved | [4] | ||
| Synonyms |
Torisel
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| MOA | Inhibitor | |||
| Activity | IC50 = 1760 nM | |||
| External Link | ||||
| Everolimus | Approved | [5] | ||
| Synonyms |
Afinitor; Afinitor (TN); CERTICAN(R); Certican; Certican (TN); Everolimus (JAN/USAN/INN); Everolimus [USAN]; MTOR kinase inhibitors; NVP-RAD-001; RAD 001; RAD-001; RAD-001C; RAD001; RAD001, SDZ-RAD, Certican, Zortress, Afinitor, Everolimus; SDZ-RAD; Zortress
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| MOA | Inhibitor | |||
| External Link | ||||
| Zotarolimus | Approved | [6] | ||
| Synonyms |
Abt-578; Zotarolimus (TN)
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| MOA | Modulator | |||
| Activity | IC50 = 3.3 nM | |||
| External Link | ||||
| Sirolimus | Approved | [7] | ||
| Synonyms |
53123-88-9; Rapamune; Rapamycin (Sirolimus); AY-22989; Rapammune; sirolimusum; WY-090217; RAPA; Antibiotic AY 22989; AY 22989; UNII-W36ZG6FT64; CCRIS 9024; CHEBI:9168; SILA 9268A; W36ZG6FT64; HSDB 7284; C51H79NO13; NSC 226080; DE-109; NCGC00021305-05; DSSTox_CID_3582; DSSTox_RID_77091; DSSTox_GSID_23582; Cypher; Supralimus; Wy 090217; Perceiva; RAP; RPM; Rapamycin from Streptomyces hygroscopicus; SIIA 9268A; LCP-Siro; MS-R001; Rapamune (TN); Rapamycin (TN); Sirolimus (RAPAMUNE); Rapamycin C-7, analog 4; Sirolimus (USAN/INN); Sirolimus [USAN:BAN:INN]; Sirolimus, Rapamune,Rapamycin; Heptadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy; 23,27-Epoxy-3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine; 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine; 23,27-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine-1,5,11,28,29; 3H-pyrido(2,1-c)(1,4)oxaazacyclohentriacontine-1,5,11,28,29(4H,6H,31H)-pentone; Sirolimus (MTOR inhibitor)
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| MOA | Inhibitor | |||
| External Link | ||||
| PF-04449913 | Approved | [8] | ||
| Synonyms |
Glasdegib; 1095173-27-5; PF 04449913; UNII-K673DMO5H9; K673DMO5H9; CHEMBL2043437; Glasdegib (PF-04449913); Glasdegib [USAN:INN]; Glasdegib (USAN/INN); PF-04449913;Glasdegib; GTPL8201; Glasdegib(PF-04449913); EX-A858; MolPort-035-789-706; SFNSLLSYNZWZQG-VQIMIIECSA-N; ZINC68251434; PF-913; BDBM50385635; 2640AH; AKOS027324121; CS-2
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| MOA | Inhibitor | |||
| External Link | ||||
| Ridaforolimus | Phase 3 | [9] | ||
| Synonyms |
Deforolimus; AP 23573; MK 8669; AP-23573; MK-8669; AP23573, MK-8669, Ridaforolimus, Deforolimus
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| MOA | Inhibitor | |||
| External Link | ||||
| INK128 | Phase 2 | [10] | ||
| Synonyms |
1224844-38-5; Sapanisertib; INK-128; INK 128; INK 128 (MLN0128); TAK-228; UNII-JGH0DF1U03; JGH0DF1U03; 5-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)benzo[d]oxazol-2-amine; INK-0128; 3-(2-Amino-5-benzoxazolyl)-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; C15H15N7O; 5-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)-1,3-benzoxazol-2-amine; 5-(4-Amino-1-isopropyl-1H-pyrazolo[3,4-d]-pyrimidin-3-yl)benzo[d]oxazol-2-amine; Sapanisertib (USAN/INN)
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| MOA | Inhibitor | |||
| Activity | Ki = 1 nM | |||
| External Link | ||||
| OSI-027 | Phase 2 | [11] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| ABI-009 | Phase 2 | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Salirasib | Discontinued in Phase 1/2 | [3] | ||
| Synonyms |
162520-00-5; Farnesylthiosalicylic acid; S-Farnesylthiosalicylic acid; UNII-MZH0OM550M; MZH0OM550M; CHEMBL23293; AK186909; Farnesyl Thiosalicylic Acid; 2-[[(2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrien-1-yl]thio]benzoic Acid; 2-[(2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienyl]sulfanylbenzoic acid; 2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)benzoic acid; 2-(((2E,6E)-3,7,11-Trimethyl-2,6,10-dodecatrienyl)sulfanyl)benzoic acid; Benzoic acid, 2-(((2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrienyl)thio)-; FTS; Farnesylthiosalicyclic acid; FTS, Thyreos; Ras antagonists, Thyreos; S-trans; Th-101; Trans-farnesylthiosalicylicacid; FTS (oral, cancer), Concordia; Farnesylthiosalicyclic acid (oral, cancer), Concordia; Ras-inhibitors (cancer), Concordia; FTS (oral, cancer), Concordia/Ono; KD032
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| MOA | Modulator | |||
| External Link | ||||
| SAR245409 | Phase 2 | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 157 nM | |||
| External Link | ||||
| SF1126 | Phase 2 | [12] | ||
| Synonyms |
CC-1126; SF-1126; L-Serine, N2-(1,4-dioxo-4-((4-(4-oxo-8-phenyl-4H-1-benzopyran-2-yl)morpholinium-4-yl)methoxy)butyl)-L-arginylglycyl-L-alpha-aspartyl-, inner salt
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| MOA | Inhibitor | |||
| External Link | ||||
| PF-05212384 | Phase 2 | [13] | ||
| Synonyms |
PKI-587; 1197160-78-3; Gedatolisib; PKI587; PKI 587; 1-(4-(4-(Dimethylamino)piperidine-1-carbonyl)phenyl)-3-(4-(4,6-dimorpholino-1,3,5-triazin-2-yl)phenyl)urea; PF 05212384; UNII-96265TNH2R; PF-05212384 (PKI-587); CHEMBL592445; 96265TNH2R; N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea; Gedatolisib (PF-05212384, PKI-587); Urea, N-(4-((4-(dimethylamino)-1-piperidinyl)carbonyl)phenyl)-N'-(4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl)-
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| MOA | Modulator | |||
| Activity | IC50 = 0.4 nM | |||
| External Link | ||||
| LY3023414 | Phase 2 | [14] | ||
| MOA | Modulator | |||
| External Link | ||||
| PF-04691502 | Phase 2 | [15] | ||
| Synonyms |
1013101-36-4; PF 04691502; UNII-4W39NS61KI; 4W39NS61KI; 2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one; CHEMBL1234354; PF04691502; 2-Amino-8-[trans-4-(2-Hydroxyethoxy)cyclohexyl]-6-(6-Methoxypyridin-3-Yl)-4-Methylpyrido[2,3-D]pyrimidin-7(8h)-One; 2-Amino-8-[4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7-one
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| MOA | Modulator | |||
| Activity | IC50 = 7.9 nM | |||
| External Link | ||||
| GDC-0980/RG7422 | Phase 2 | [3] | ||
| Synonyms |
Apitolisib; 1032754-93-0; GDC-0980; GDC0980; RG7422; (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one; UNII-1C854K1MIJ; GDC-0980 (RG7422); Apitolisib (GDC-0980, RG7422); 1C854K1MIJ; CHEMBL1922094; RG-7422; (2s)-1-(4-{[2-(2-Aminopyrimidin-5-Yl)-7-Methyl-4-(Morpholin-4-Yl)thieno[3,2-D]pyrimidin-6-Yl]methyl}piperazin-1-Yl)-2-Hydroxypropan-1-One; J-502360; C23H30N8O3S
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| MOA | Modulator | |||
| Activity | Ki = 17 nM | |||
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| BEZ235 | Phase 2 | [16] | ||
| Synonyms |
BEZ-235; S14-0511; NVP-BEZ-235; NVP-BEZ235, BEZ235; 2-(4-(2,3-dihydro-3-methyl-2-oxo-8-(quinolin-3-yl)imidazo[4,5-c]quinolin-1-yl)phenyl)-2-methylpropanenitrile
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| MOA | Modulator | |||
| Activity | IC50 = 5 nM | |||
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| MM-141 | Phase 2 | [12] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PQR309 | Phase 2 | [3] | ||
| Synonyms |
Bimiralisib; 1225037-39-7; PI3K-IN-2; PQR-309; UNII-6Z3QHB00LB; 6Z3QHB00LB; 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; 5-[bis(morpholin-4-yl)-1,3,5-triazin-2-yl]-4-(trifluoromethyl)pyridin-2-amine; 5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine; Bimiralisib [INN]; Bimiralisib [USAN]; Bimiralisib [WHO-DD]; NCB5; SCHEMBL1309049; GTPL8383; Bimiralisib free base; ADGGYDAFIHSYFI-UHFFFAOYSA-N; EX-A2018; BCP15887; PQR-309(PI3K-IN-2)
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| MOA | Inhibitor | |||
| Activity | Ki = 62 nM | |||
| External Link | ||||
| AZD2014 | Phase 2 | [17] | ||
| Synonyms |
1009298-59-2; Vistusertib; AZD-2014; AZD 2014; UNII-0BSC3P4H5X; 0BSC3P4H5X; cc-551; 3-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[5,6-e]pyrimidin-7-yl]-N-methylbenzamide; CHEMBL2336325; 3-[2,4-Bis((3S)-3-methyLmorpholin-4-yl)pyrido-[5,6-e]pyrimidin-7-yl]-N-methylbenzamide; C25H30N6O3; 3-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-N-methylbenzamide; 3-[2,4-bis[(3S)-3-methylmorpholin-4-yl]pyrido[2,3-d]pyrimidin-7-yl]-N-methylbenzamide; Vistusertib [INN]; Vistusertib [USAN]; Vistusertib (JAN/INN)
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| MOA | Inhibitor | |||
| Activity | IC50 = 2.8 nM | |||
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| CC-223 | Phase 1/2 | [18] | ||
| Synonyms |
GW 791343 HYDROCHLORIDE; GW791343 trihydrochloride; 309712-55-8; 1019779-04-4; GW791343 HCl; GW791343 (trihydrochloride); GW791343; GW-791343; 2-[(3,4-Difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]-acetamide trihydrochloride; GW791343 (HCL); GW-791343 hydrochloride; C20H27Cl3F2N4O; GW 791343 Trihydrochloride; C20H24F2N4O.3ClH; CTK8F0044; EX-A438; GW 791343 HCl; WSBRAHWNJBXXJM-UHFFFAOYSA-N; MolPort-023-219-209; BCP23425; AKOS024457596; CS-1030; BCP9000749; API0008007; HY-15470; BCP0726000290; RT-017402; KB-272661
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| MOA | Modulator | |||
| Activity | IC50 = 10 nM | |||
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| BGT226 | Phase 1/2 | [19] | ||
| Synonyms |
BGT-226 free base; 915020-55-2; UNII-ZXE7F2GMJJ; BGT226 free base; ZXE7F2GMJJ; BGT-226; 8-(6-Methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-trifluoromethylphenyl]-1,3-dihydroimidazo[4,5-c]quinolin-2-one; CHEBI:71967; BGT 226; NVPBGT226; 8-(6-methoxypyridin-3-yl)-3-methyl-1-[4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one; 8-(6-Methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one; NPV-BGT226; SCHEMBL146939
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| MOA | Modulator | |||
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| ME-344 | Phase 1/2 | [20] | ||
| Synonyms |
NV-128; NV-344; MTOR inhibitor (cancer), Novogen; MTOR inhibitors (cancer), Marshall Edwards
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| MOA | Inhibitor | |||
| External Link | ||||
| BI 860585 | Phase 1 | [21] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| LAM-001 | Phase 1 | [22] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| DS-3078 | Phase 1 | [23] | ||
| MOA | Modulator | |||
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| GDC-0349 | Phase 1 | [24] | ||
| Synonyms |
MTORC1/2 inhibitors
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| MOA | Inhibitor | |||
| Activity | Ki = 3.8 nM | |||
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| CERC 006 | Phase 1 | [25] | ||
| Synonyms |
(+/-)-Cyclohexanecarboxylic acid, 4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo(5,1-f)(1,2,4)triazin-7-yl)-, trans-; (1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexane-1-carboxylic acid; (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; (1r,4r)-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo-[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; 1187559-66-5; 25MKH1SZ0M; 4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f] [1,2,4]Triazin-7-yl)cyclohexanecarboxylic Acid; 4-[(5Z)-4-amino-5-(7-methoxyindol-2-ylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexane-1-carboxylic acid; 4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]cyclohexane-1-carboxylic acid; 4-[4-amino-5-(7-methoxy-2-indolylidene)-1H-imidazo[5,1-f][1,2,4]triazin-7-yl]-1-cyclohexanecarboxylic acid; 936890-98-1; 936890-98-1 (free acid); A-1065; AC-31517; AEVI-006; AKOS030238938; AKOS037643584; AM81260; AS-17003; ASP 7486; ASP4786; ASP7486; ASP-7486; BCP02613; BCP9001034; BDBM185151; BRD-K94294671-003-01-3; CCG-268721; CERC 006; CERC006; CERC-006; CHEBI:91363; CHEMBL2132692; CHEMBL3120215; CS-0257; Cyclohexanecarboxylic acid, 4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo(5,1-f)(1,2,4)triazin-7-yl)-, trans-; Cyclohexanecarboxylic acid, 4-[4-amino-5-(7-methoxy-1h-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-, trans-; DB12387; DTXSID901025951; EX-A143; F17371; HMS3656H05; HMS3748I11; HY-10423; J-523839; JROFGZPOBKIAEW-HAQNSBGRSA-N; LS-14875; MLS006011006; NCGC00250395-01; NCGC00386179-01; NCGC00386179-04; NCGC00387858-03; NSC800810; NSC-800810; OSI 027; OSI027; OSI-027; Q27163231; Q27253978; s2624; SB19259; SCHEMBL20482333; SCHEMBL22594988; SCHEMBL22787096; SCHEMBL976795; SCHEMBL976796; SMR004702804; SW220246-1; trans-4-(4-Amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid; TRANS-4-[4-AMINO-5-(7-METHOXY-1H-INDOL-2-YL)IMIDAZO[5,1-F][1,2,4]TRIAZIN-7-YL]CYCLOHEXANECARBOXYLIC ACID; trans-4-[4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl]-cyclohexanecarboxylic acid; trans-4-[4-amino-5-(7-methoxy-1H-indol-2-yl)-imidazo[5,1-f][1,2,4]triazin-7-yl]-cyclohexanecarboxylic acid; UNII-25MKH1SZ0M
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| MOA | Inhibitor | |||
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| DS-7423 | Phase 1 | [26] | ||
| MOA | Modulator | |||
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| PWT-33597 | Phase 1 | [27] | ||
| Synonyms |
PI3 kinase alpha/mTOR dual inhibitor (cancer), Pathway Therapeutics
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| MOA | Modulator | |||
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| VS-5584 | Phase 1 | [3] | ||
| Synonyms |
5-(9-Isopropyl-8-methyl-2-morpholino-9H-purin-6-yl)pyrimidin-2-amine; 1246560-33-7; VS-5584 (SB2343); UNII-W71J4X250V; SB-2343; SB2343; CHEMBL3393066; W71J4X250V; 5-(8-methyl-2-morpholin-4-yl-9-propan-2-ylpurin-6-yl)pyrimidin-2-amine; C17H22N8O; QYBGBLQCOOISAR-UHFFFAOYSA-N; SCHEMBL539098; GTPL8382; EX-A288; DTXSID10677328; MolPort-035-757-944; HMS3652B16; BCP08247; 2797AH; ZINC95644685; s7016; VS5584; BDBM50059635; AKOS024465057; 5-(9-isopropyl-8-methyl-2-morpholin-4-yl-9H-purin-6-yl)-pyrimidin-2-ylamine; SB16877
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| MOA | Modulator | |||
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| PMID25726713-Compound-49 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-51 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
| External Link | ||||
| PMID25726713-Compound-48 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-47 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
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| PMID25726713-Compound-50 | Patented | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1 nM | |||
| External Link | ||||
| AZD8055 | Discontinued in Phase 1/2 | [29] | ||
| Synonyms |
1009298-09-2; AZD-8055; AZD 8055; [5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol; (5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol; UNII-970JJ37FPW; 970JJ37FPW; CHEMBL1801204; AK109550; (5-(2,4-Bis((S)-3-methylmorpholino)pyrido-[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol; (5-(2,4-bis((3S)-3-methylmorpholin-4-yl)pyrido(2,3-d)pyrimidin-7-yl)-2-methoxyphenyl)methanol
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| MOA | Inhibitor | |||
| Activity | IC50 = 4 nM | |||
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| TAFA-93 | Discontinued in Phase 1 | [30] | ||
| Synonyms |
MTOR inhibitor, Isotechnika; Rapamycin prodrug, Isotechnika; Transplant rejection therapy, Isotechnika
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| MOA | Inhibitor | |||
| External Link | ||||
| SCR-44001 | Terminated | [31] | ||
| Synonyms |
MTOR pathway inhibitors (cancer); PI3K modulators, BioImage; SCR-0044001; SCR-0334654; SCR-0335319; TOP-216; MTOR pathway inhibitors (cancer), TopoTarget; MTOR pathway inhibitors (cancer), BioImage/TopoTarget
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| MOA | Inhibitor | |||
| External Link | ||||
| (4-(6-morpholino-9H-purin-2-yl)phenyl)methanol | Investigative | [32] | ||
| Synonyms |
CHEMBL594669; SCHEMBL4442909
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| MOA | Inhibitor | |||
| Activity | IC50 = 4500 nM | |||
| External Link | ||||
| Rapamycin complexed with immunophilin FKBP12 | Investigative | [33] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| C-16-(S)-3-methylindolerapamycin | Investigative | [34] | ||
| Synonyms |
CHEMBL503885
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| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PF-05094037 | Investigative | [3] | ||
| Synonyms |
PF-05171310; PF-05181059; MTOR inhibitors (cancer), Pfizer
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| MOA | Inhibitor | |||
| External Link | ||||
| SX-MTR1 | Investigative | [3] | ||
| Synonyms |
MTOR modulators (small peptide mimetics, bladder cancer), Serometrix
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| MOA | Modulator | |||
| External Link | ||||
| 2-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2500 nM | |||
| External Link | ||||
| P-2281 | Investigative | [3] | ||
| Synonyms |
MTOR inhibitor (ulcerative colitis), Piramal
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| MOA | Inhibitor | |||
| External Link | ||||
| X-387 | Investigative | [3] | ||
| Synonyms |
MTOR inhibitors (cancer), Shanghai Institute of Materia Medica
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 450 nM | |||
| External Link | ||||
| EM-101 | Investigative | [3] | ||
| Synonyms |
EM-100 series; LY-3; LY-303511; MTOR pathway inhibitors (cancer), Emiliem; MTOR pathway inhibitors (cancer), NIH
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| MOA | Inhibitor | |||
| External Link | ||||
| EC-0845 | Investigative | [3] | ||
| Synonyms |
MTOR modulator (inflammatory disease), Endocyte
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| MOA | Modulator | |||
| External Link | ||||
| 4-(2-(thiophen-2-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL604876; SCHEMBL4439490
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| MOA | Inhibitor | |||
| Activity | IC50 = 2800 nM | |||
| External Link | ||||
| SB-2280 | Investigative | [3] | ||
| Synonyms |
SB-2602; Selective mTOR inhibitors (cancer); Selective mTOR inhibitors (cancer), S*BIO
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| MOA | Inhibitor | |||
| External Link | ||||
| 4-(2-(thiophen-3-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL608095; SCHEMBL4438208
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| MOA | Inhibitor | |||
| Activity | IC50 = 3900 nM | |||
| External Link | ||||
| torin 1 | Investigative | [35] | ||
| Synonyms |
Torin-1
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| MOA | Inhibitor | |||
| Activity | IC50 = 4.32 nM | |||
| External Link | ||||
| EC-0565 | Investigative | [3] | ||
| Synonyms |
Folate-everolimus conjugate (inflammation), Endocyte
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| MOA | Inhibitor | |||
| External Link | ||||
| OXA-01 | Investigative | [3] | ||
| Synonyms |
MTORC1/mTORC2 inhibitor (cancer) OSI Pharmaceuticals
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| MOA | Inhibitor | |||
| External Link | ||||
| AR-mTOR-26 | Investigative | [3] | ||
| Synonyms |
AR-mTOR-1; MTORC1/2 inhibitors (cancer); MTORC1/2 inhibitors (cancer), Array BioPharma
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-chloro-N-(6-cyanopyridin-3-yl)propanamide | Investigative | [36] | ||
| Synonyms |
1112994-35-0; SCHEMBL1483919; CHEMBL446834; VFOLQYOVUCHHET-UHFFFAOYSA-N
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| MOA | Inhibitor | |||
| External Link | ||||
| 3-(6-morpholino-9H-purin-2-yl)phenol | Investigative | [32] | ||
| Synonyms |
CHEMBL593515; SCHEMBL4443377; FUDQNOGEMXSUSQ-UHFFFAOYSA-N
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| MOA | Inhibitor | |||
| Activity | IC50 = 1650 nM | |||
| External Link | ||||
| AP-21967 | Investigative | [34] | ||
| Synonyms |
CHEMBL525042; SCHEMBL18176922; C-16-(S)-7-methylindolerapamycin
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| 4-(2-(1H-indol-6-yl)-9H-purin-6-yl)morpholine | Investigative | [32] | ||
| Synonyms |
CHEMBL611630
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| MOA | Inhibitor | |||
| Activity | IC50 = 150 nM | |||
| External Link | ||||
| Torin2 | Investigative | [37] | ||
| Synonyms |
Torin 2; 1223001-51-1; Torin-2; 9-(6-aminopyridin-3-yl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one; 9-(6-AMINO-3-PYRIDINYL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-BENZO[H]-1,6-NAPHTHYRIDIN-2(1H)-ONE; CHEMBL1765602; C24H15F3N4O; CHEBI:90682; 9-(6-Aminopyridin-3-Yl)-1-[3-(Trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2(1h)-One; 9-(6-AMINOPYRIDIN-3-YL)-1-(3-(TRIFLUOROMETHYL)PHENYL)BENZO[H][1,6]NAPHTHYRIDIN-2(1H)-ONE; 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)-phenyl)benzo[h][1,6]naphthyridin-2(1H)-one; BENZO[H]-1,6-NAPHTHYRIDIN-2(1H)-ONE, 9-(6-AMINO-3-PYRIDINYL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-; 9-(6-Amino-3-pyridinyl)-1-[3-(trifluoromethyl)phenyl]benzo[h]-1,6-naphthyridin-2(1H)-one; cc-275; MLS006011167; GTPL8839; SCHEMBL6876328; AOB3537; DTXSID00679917; EX-A431; HMS3265O05; HMS3265O06; HMS3265P05; HMS3265P06; HMS3651N13; BCP02612; ABP000908; BDBM50341209; MFCD18782652; NSC775727; s2817; ZINC71318831; AKOS024458055; CCG-265003; CS-0236; NSC-775727; PB34957; NCGC00263216-01; NCGC00263216-02; NCGC00263216-09; NCGC00263216-13; 9-(6-AMINO-PYRIDIN-3-YL)-1-(3-TRIFLUOROMETHYL-PHENYL)-1H-BENZO[H][1,6]NAPHTHYRIDIN-2-ONE; AC-31520; AK171126; AS-74405; HY-13002; SMR004702936; AB0035864; DB-084736; FT-0700124; SW218309-2; Y0293; Q-4148; J-519481; BRD-K68174511-001-01-7; Q27089008; 9-(6-amino-3-pyridyl)-1-[3-(trifluoromethyl)phenyl]benzo[h][1,6]naphthyridin-2-one; 17G; 9-(6-Amino-3-pyridinyl)-1-[3-(trifl uoromethyl)phenyl]-benzo[h]-1,6-naphthyridin-2(1H) -one; 9-(6-AMINOPYRIDIN-3-YL)-1-[3-(TRIFLUOROMETHYL)PHENYL]-1H,2H-BENZO[H]1,6-NAPHTHYRIDIN-2-ONE
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| MOA | Inhibitor | |||
| External Link | ||||
| HM-5016699 | Investigative | [3] | ||
| Synonyms |
Dual PI3K/mTOR inhibitor (cancer); Dual PI3K/mTOR inhibitor (cancer), Hutchison
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| MOA | Inhibitor | |||
| External Link | ||||
| PF-03772304 | Investigative | [38] | ||
| Synonyms |
MTOR inhibitors, Biotica; MTOR inhibitors, Wyeth; PF-04979064; PF-05017255; PF-05168899; WYE-125132; WYE-132; WYE-178; WYE-354; WYE-600; WYE-687; Imidazolo and pyrazolopyrimidine derivatives (cancer), Pfizer; Imidazolopyrimidine derivatives (cancer), Pfizer; Imidazolopyrimidine derivatives (cancer), Wyeth; Non-rapamycin mTOR/PI3K inhibitors (cancer); PI3K/mTOR signalling inhibitors (cancer), Wyeth; Non-rapamycin mTOR/PI3K inhibitors (cancer), Pfizer; 5H-pyrrolo[3,2-d]pyridimine analogs (cancer), Wyeth
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| MOA | Inhibitor | |||
| External Link | ||||
| PP-242 | Investigative | [39] | ||
| Synonyms |
PP242; TORKinib
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| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
| External Link | ||||
| CU-906 | Investigative | [3] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| P-6915 | Investigative | [3] | ||
| Synonyms |
PI3K/mTOR inhibitors (cancer), Piramal
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| MOA | Inhibitor | |||
| External Link | ||||
| 2-Morpholin-4-yl-pyrimido[2,1-a]isoquinolin-4-one | Investigative | [40] | ||
| Synonyms |
Compound 401; 168425-64-7; 2-morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one; 2-(morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one; CHEMBL179242; 2-(4-MORPHOLINYL)-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE; Compound401; SCHEMBL10092321; KS-00001DEG; CTK4D2994; DTXSID20434626; MolPort-023-276-726; HMS3229D15; EX-A1016; BCP04303; BDBM50159620; ZINC13608047; AKOS016369524; CS-5624; NCGC00378805-02; HY-19341; KB-224235; M2537; B7337; S-7713; J-010456
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| MOA | Inhibitor | |||
| Activity | IC50 = 5300 nM | |||
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| 2-(2-Methyl-morpholin-4-yl)-benzo[h]chromen-4-one | Investigative | [40] | ||
| Synonyms |
CHEMBL435507; SCHEMBL3545107
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| MOA | Inhibitor | |||
| Activity | IC50 = 4800 nM | |||
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| Ethyl 1-[(1H-benzimidazol-2(3H)one-5-yl)sulfonyl]-1H-pyrrole-2-carboxylate | Investigative | [40] | ||
| Synonyms |
2-(Morpholin-4-yl)-benzo[h]chromen-4-one; 154447-35-5; NU7026; NU 7026; DNA-PK Inhibitor II; NU-7026; 2-morpholino-4H-benzo[h]chromen-4-one; LY293646; LY-293646; 2-(4-Morpholinyl)-4H-naphthol[1,2-b]pyran-4-one; 2-(4-morpholinyl)-4H-naphtho[1,2-b]pyran-4-one; CHEMBL104468; AK186905; DNA-Dependent Protein Kinase Inhibitor II; 2-morpholin-4-ylbenzo[h]chromen-4-one; SCHEMBL610237; ZINC9230; GTPL5959; KS-00000XHI; CTK0E7833; CHEBI:92165; DTXSID10432010; AOB2835; MolPort-009-019-548; HMS3229C11; EX-A1100; BCP04736; IN1364; s2893
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| MOA | Inhibitor | |||
| Activity | IC50 = 6400 nM | |||
| External Link | ||||
| PP121 | Investigative | [39] | ||
| Synonyms |
PP-121; PP 121
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| 2C25: Lung cancer | 52 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Adagrasib | Approved | [41] | ||
| Synonyms |
2326521-71-3; MRTX-849; UNII-8EOO6HQF8Y; 8EOO6HQF8Y; 2-((S)-4-(7-(8-Chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; CHEMBL4594350; SCHEMBL20974691; GTPL10888; Kras G12C inhibitor MRTX849; BCP31538; EX-A3258; MRTX 849; MFCD32263433; s8884; compound 20 [PMID: 32250617]; BS-16211; HY-130149; CS-0105265; 2-Piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-
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| Amivantamab | Approved | [42] | ||
| External Link | ||||
| Mobocertinib | Approved | [43] | ||
| Synonyms |
1847461-43-1; TAK-788; TAK788; AP32788; UNII-39HBQ4A67L; 39HBQ4A67L; propan-2-yl 2-[4-{[2-(dimethylamino)ethyl](methyl)amino}-2-methoxy-5-(prop-2-enamido)anilino]-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Mobocertinib [INN]; Mobocertinib [USAN]; AP-32788; Mobocertinib (TAK788); Mobocertinib(TAK-788); SCHEMBL17373133; GTPL10468; BDBM368374; BCP31045; EX-A3392; US10227342, Example 10; MFCD32669806; NSC825519; s6813; TAK-788;AP32788; WHO 11183; NSC-825519; example 94 [WO2015195228A1]; HY-135815; CS-0114256; TAK-788;TAK 788; AP 32788; 5-Pyrimidinecarboxylic acid, 2-((4-((2-(dimethylamino)ethyl)methylamino)-2-methoxy-5-((1-oxo-2-propen-1-yl)amino)phenyl)amino)-4-(1-methyl-1H-indol-3-yl)-, 1-methylethyl ester; C(C=C)(=O)NC=1C(=CC(=C(C=1)NC1=NC=C(C(=N1)C1=CN(C2=CC=CC=C12)C)C(=O)OC(C)C)OC)N(C)CCN(C)C; Isopropyl 2-((5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)amino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Isopropyl 2-(5-acrylamido-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenylamino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; Propan-2-yl 2-(5-(acryloylamino)-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyanilino)-4-(1-methyl-1H-indol-3-yl)pyrimidine-5-carboxylate; propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate
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| Sugemalimab | Approved in China | [44] | ||
| External Link | ||||
| Sacituzumab govitecan | Approved | [45] | ||
| Synonyms |
1491917-83-9; 1535963-91-7; 1796566-95-4; CYSTEINYL CL2A-SN-38; DA64T2C2IO; DTXSID401335985; EX-A4354; F82944; GOVITECAN CYSTEINYL CONJUGATE; hRS 7SN38; hRS7-SN38; IMMU 132; IMMU-132; M9BYU8XDQ6; Sacituzumab govitecan; Sacituzumab govitecan [USAN]; sacituzumab-govitecan; Satralizumab linker; SN-38 CYSTEINYL CONJUGATE; UNII-M9BYU8XDQ6
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| Atezolizumab | Approved | [46] | ||
| External Link | ||||
| Tepotinib | Approved | [47] | ||
| Synonyms |
1100598-32-0; EMD 1214063; UNII-1IJV77EI07; Tepotinib (EMD 1214063); EMD1214063; 1IJV77EI07; MSC-2156119J; Benzonitrile, 3-[1,6-dihydro-1-[[3-[5-[(1-methyl-4-piperidinyl)methoxy]-2-pyrimidinyl]phenyl]methyl]-6-oxo-3-pyridazinyl]-; C29H28N6O2; Tepotinib [INN]; Benzonitrile, 3-[1,6-Dihydro-1-[[3-[5-[(1-Methyl-4-Piperidinyl)Methoxy]-2-PyriMidinyl]Phenyl]Methyl]-6-Oxo-3-Pyridazinyl]; Benzonitrile, 3-(1,6-dihydro-1-((3-(5-((1-methyl-4-piperidinyl)methoxy)-2-pyrimidinyl)phenyl)methyl)-6-oxo
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| External Link | ||||
| Sotorasib | Approved | [48] | ||
| Synonyms |
AMG-510; AMG510; AMG-510 racemate; 2252403-56-6; AMG 510; Kras G12C inhibitor 9; 2296729-00-3; UNII-2B2VM6UC8G; 2B2VM6UC8G; CHEMBL4535757; 2296729-00-3 (racemate); 4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one; Sotorasib [INN]; 6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-((2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl)pyrido(2,3-d)pyrimidin-2-one; AMG510 racemate; Sotorasib [USAN]; AMG-510(racemate); Kras mutant-targeting AMG 510; SCHEMBL20560375; GTPL10678; AMG 510 pound>>AMG-510; AMY16918; BCP30452; BCP33368; EX-A3538; BDBM50514402; NSC818433; s8830; WHO 11370; DB15569; NSC-818433; BS-16684; HY-114277; CS-0081316; compound (R)-38 [PMID: 31820981]; (1m)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(propan-2-yl)pyridin-3-yl)-4-((2S)-2-methyl-4-(prop-2-enoyl)piperazin-1-yl)pyrido(2,3-d)pyrimidin-2(1H)-one; (1S)-4-((S)-4-Acryloyl-2-methylpiperazin-1-yl)-6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(2-isopropyl-4-methylpyridin-3-yl)pyrido[2,3-d]pyrimidin-2(1H)-one; 2296729-66-1; Pyrido(2,3-d)pyrimidin-2(1H)-one, 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(1-methylethyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(1-oxo-2-propen-1-yl)-1-piperazinyl)-
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| Entrectinib | Approved | [49] | ||
| Synonyms |
1108743-60-7; RXDX-101; UNII-L5ORF0AN1I; Entrectinib (RXDX-101); L5ORF0AN1I; Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-; Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-; Entrectinib [USAN:INN]; YMX; Kinome_2659; Entrectinib(rxdx-101); Entrectinib (USAN/INN); SCHEMBL3512601; GTPL8290; CHEMBL1983268; KS-00000TSK
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| Repotrectinib | Approved | [50] | ||
| Synonyms |
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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| MYL-1402O | Phase 3 | [51] | ||
| Synonyms |
bevacizumab biosimilar
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| AB154 | Phase 3 | [52] | ||
| Synonyms |
Domvanalimab
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| Datopotamab deruxtecan | Phase 3 | [53] | ||
| External Link | ||||
| CS1001 | Phase 3 | [54] | ||
| External Link | ||||
| JDQ443 | Phase 3 | [55] | ||
| Synonyms |
(S)-JDQ-443; 1-(6-((4S)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one; 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-inda zol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]- 2-Propen-1-one; 1-[6-[(4R)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-2-propen-1-one; 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one; 1-{6-[(4M)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5- methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2- azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 1-{6-[(4M)-4-(5-Chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl}prop-2-en-1-one; 2653994-08-0; 2653994-10-4; 2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-; AKOS040757949; AT36708; BDBM50579985; CHEMBL5077861; compound 5 [PMID: 35404998]; CS-0226220; CS-0311034; EX-A5693; example 1a [WO2021120890A1]; GLXC-25533; GTPL11715; HY-139612A; JDQ 443; JDQ 443 [WHO-DD]; JDQ443; JDQ-443; MS-29737; NSC846146; NSC-846146; NVP-JDQ443; NVP-JDQ-443; Opnurasib; opnurasib [INN]; -PROPEN-1-ONE, 1-(6-((4R)-4-(5-CHLORO-6-METHYL-1H-INDAZOL-4-YL)-5-METHYL-3-(1-METHYL-1H-INDAZOL-5-YL)-1H-PYRAZOL-1-YL)-2-AZASPIRO(3.3)HEPT-2-YL)-; Q3W0H3V1LQ; SCHEMBL23533580
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| TRS003 | Phase 3 | [56] | ||
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| Tusamitamab ravtansine | Phase 3 | [57] | ||
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SAR408701
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| RG6058 | Phase 3 | [58] | ||
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Tiragolumab
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| GSK4069889 | Phase 2 | [59] | ||
| Synonyms |
TSR-022
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| APL-101 | Phase 2 | [60] | ||
| Synonyms |
Bozitinib; PLB-1001; 1440964-89-5; Vebreltinib; Vebreltinib [USAN]; UNII-2WZP8A9VFN; 2WZP8A9VFN; Bozitinib (PLB-1001); SCHEMBL15594471; BDBM107096; CBI-3103; s6762; WHO 11677; HY-125017; CS-0088607; US9695175, 44; 1,2,4-Triazolo(4,3-b)pyridazine, 6-(1-cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6- fluoro-2-methyl-2H-indazol-5-yl)methyl)-; 6-(1-Cyclopropyl-1H-pyrazol-4-yl)-3-(difluoro(6-fluoro-2-methyl-2H-indazol-5- yl)methyl)-1,2,4-triazolo(4,3-b)pyridazine
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| SGN-LIV1A | Phase 2 | [61] | ||
| Synonyms |
Ladiratuzumab Vedotin
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| BNT116 | Phase 2 | [62] | ||
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| AZD7789 | Phase 2 | [63] | ||
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| L-DOS47 | Phase 1/2 | [64] | ||
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| NC318 | Phase 2 | [65] | ||
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| Vorolanib | Phase 2 | [66] | ||
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UNII-YP8G3I74EL; YP8G3I74EL; 1013920-15-4; (S,Z)-N-(1-(Dimethylcarbamoyl)pyrrolidin-3-yl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; Vorolanib [INN]; SCHEMBL2439528; CHEMBL4297587; N-((3S)-1-(dimethylcarbamoyl)pyrrolidin-3-yl)-5-((Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide; s6843; DB15247; HY-109019; CS-0030517; Q27294638; 1H-Pyrrole-3-carboxamide, N-((3S)-1-((dimethylamino)carbonyl)-3-pyrrolidinyl)-5-((Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl)-2,4-dimethyl-
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| Xofigo | Phase 2 | [67] | ||
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| Bintrafusp alfa | Phase 2 | [68] | ||
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| Voyager-V1 | Phase 2 | [69] | ||
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VSV-IFNBeta-NIS
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| AB-106 | Phase 2 | [70] | ||
| Synonyms |
DS6051b; GTPL11198; AB106
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| RO-5126766 | Phase 2 | [71] | ||
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VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TC-210 | Phase 1/2 | [72] | ||
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| EMB-01 | Phase 1/2 | [73] | ||
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| NM21-1480 | Phase 1/2 | [74] | ||
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| MRx0518 | Phase 1/2 | [75] | ||
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| DZD9008 | Phase 1/2 | [76] | ||
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| BGB-A425 | Phase 1/2 | [77] | ||
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| Rilvegostomig | Phase 1/2 | [78] | ||
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AZD2936
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| IK-007 | Phase 1/2 | [79] | ||
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grapiprant
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| IBI318 | Phase 1 | [80] | ||
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| GEN-011 | Phase 1 | [81] | ||
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| ENV-105 | Phase 1 | [82] | ||
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Carotuximab
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| AMG 160 | Phase 1 | [83] | ||
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| ADP-A2M10 | Phase 1 | [84] | ||
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| MEDI5752 | Phase 1 | [85] | ||
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| PF-07104091 | Phase 1 | [86] | ||
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| PF-06936308 | Phase 1 | [87] | ||
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| GEM3PSCA | Phase 1 | [88] | ||
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| PF-07257876 | Phase 1 | [89] | ||
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| Cosibelimab | Phase 1 | [90] | ||
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CK-301/TG-1501
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| Gemcitabine | Approved | [91] | ||
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| SMI-4a | Investigative | [92] | ||
| Synonyms |
438190-29-5; SMI 4a; TCS PIM-1 4a; (Z)-SMI-4a; (Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione; (5Z)-5-[3-(trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione; CHEMBL183906; (5Z)-5-[[3-(TRIFLUOROMETHYL)PHENYL]METHYLENE]-2,4-THIAZOLIDINEDIONE; (5Z)-5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione; 327033-36-3; C11H6F3NO2S; (Z)-5-(3-(Trifluoromethyl)benzylidene)-thiazolidine-2,4-dione; (5Z)-5-{[3-(trifluoromethyl)phenyl]methylidene}-1,3-thiazolidine-2,4-dione; Pim inhibitor 4a; 3vc4; SMI-4q; TCS PIM-1-4a; 5-(3-(Trifluoromethyl)benzylidene)thiazolidine-2,4-dione; 5-[3-(Trifluoromethyl)benzylidene]thiazolidine-2,4-dione; cc-717; thiazolidine-2,4-dione, 4a; SCHEMBL2541382; SCHEMBL2541388; BDBM26626; AOB6260; EX-A111; SYN1113; BDBM138364; HMS3229J21; 2720AH; HY-16576A; MFCD01152003; s8005; ZINC12576047; AKOS001314163; SMI-4a, >=98% (HPLC); CCG-265027; NCGC00345836-02; NCGC00345836-14; AC-32861; HY-15474; AB0165836; EC-000.2291; J3.561.866J; A11945; W-5256; US8877795, 12; Q27451064; 5-[[3-(trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione
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References
: m6A sites