m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03382
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[1], [2] | |||
Histone modification
H3K27ac
Epigenetic Regulator
MIR570HG
Indirect
Inhibition
m6A modification
MET
MET
METTL3
Methylation
: m6A sites
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| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | Methyltransferase-like 3 (METTL3) | WRITER | |||
| m6A Target | Hepatocyte growth factor receptor (c-Met/MET) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Regulated Target | Histone H3 lysine 27 acetylation (H3K27ac) | 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 H3K4me1 and Histone H3 lysine 27 acetylation (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 combines with Hepatocyte growth factor receptor (c-Met/MET) and causes the PI3K/AKT signalling pathway to be manipulated, which affects the sensitivity of lung cancer cells to gefitinib. METTL3 knockdown promotes apoptosis and inhibits proliferation of lung cancer cells. | ||||
| Responsed Disease | Lung cancer | ICD-11: 2C25 | |||
| Responsed Drug | Gefitinib | ||||
| Cell Process | Pyroptosis | ||||
In-vitro Model |
PC-9 | Lung adenocarcinoma | Homo sapiens | CVCL_B260 | |
| NCI-H3255 | Lung adenocarcinoma | Homo sapiens | CVCL_6831 | ||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Hepatocyte growth factor receptor (c-Met/MET) | 76 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Capmatinib | Approved | [3] | ||
| Synonyms |
1029712-80-8; INCB28060; INC-280; INC280; UNII-TY34L4F9OZ; 2-fluoro-N-methyl-4-(7-(quinolin-6-ylmethyl)imidazo[1,2-b][1,2,4]triazin-2-yl)benzamide; INC28060; INCB-28060; INCB28060(Capmatinib); NVP-INC280; TY34L4F9OZ; Capmatinib (INCB28060); INCB 28060; 2-Fluoro-N-methyl-4-[7-[(quinolin-6-yl)methyl]imidazo[1,2-b]-[1,2,4]triazin-2-yl]benzamide; BenzaMide, 2-fluoro-N-Methyl-4-[7-(6-quinolinylMethyl)iMidazo[1,2-b][1,2,4]triazin-2-yl]-; C23H17FN6O
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| MOA | Modulator | |||
| Activity | IC50 = 0.13 nM | |||
| External Link | ||||
| Tepotinib | Approved | [4] | ||
| 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
Click to Show/Hide
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| MOA | Modulator | |||
| Activity | IC50 < 1 nM | |||
| External Link | ||||
| Cabozantinib | Approved | [5] | ||
| Synonyms |
Cabometyx; Cometriq
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| MOA | Inhibitor | |||
| Activity | IC50 = 1.3 nM | |||
| External Link | ||||
| Amivantamab | Approved | [6] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Crizotinib | Approved | [7] | ||
| Synonyms |
Xalkori (TN); novel ALK inhibitors
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| MOA | Modulator | |||
| Activity | IC50 = 0.51 nM | |||
| External Link | ||||
| RG3638 | Phase 3 | [8] | ||
| Synonyms |
Onartuzumab
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| MOA | Modulator | |||
| External Link | ||||
| Savolitinib | Phase 3 | [9] | ||
| Synonyms |
1313725-88-0; AZD-6094; AZD6094; UNII-2A2DA6857R; CHEMBL3334567; 2A2DA6857R; Savolitinib [INN]; Volitinib(Savolitinib); Savolitinib [USAN:INN]; GTPL9918; SCHEMBL12489208; EX-A845; BDBM50023342; ZINC149738712; AKOS030526403; DB12048; compound 28 [PMID: 25148209]; HY-15959; AS-35250; 1H-1,2,3-Triazolo(4,5-b)pyrazine, 1-((1S)-1-imidazo(1,2-a)pyridin-6-ylethyl)-6-(1-methyl-1H-pyrazol-4-yl)-; KB-333895; FT-0700162; J-690125; 4-{1-[(1S)-1-{imidazo[1,2-a]pyri
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| MOA | Inhibitor | |||
| Activity | IC50 = 1.995 nM | |||
| External Link | ||||
| Beperminogene perplasmid | Phase 3 | [10] | ||
| MOA | Modulator | |||
| External Link | ||||
| Tivantinib | Phase 3 | [11] | ||
| Synonyms |
905854-02-6; ARQ-197; ARQ197; ARQ 197; Tivantinib (ARQ 197); (3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione; UNII-PJ4H73IL17; PJ4H73IL17; 1000873-98-2; (3R,4R)-3-(5,6-Dihydro-4H-pyrrolo(3,2,1-ij)quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione; Tivantinib [USAN:INN]; 1228508-24-4; ARQ 197, Tivantinib; Tivantinib (ARQ-197); ARQ 197 (Tivantinib); cc-86; SCHEMBL44944; Tivantinib (JAN/USAN/INN); GTPL7948; CHEMBL2103882; CHEBI:91398; QCR-102
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| MOA | Inhibitor | |||
| Activity | Ki = 355 nM | |||
| External Link | ||||
| MGCD516 | Phase 2/3 | [8] | ||
| Synonyms |
Sitravatinib
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| MOA | Inhibitor | |||
| External Link | ||||
| LY-2875358 | Phase 2 | [12] | ||
| Synonyms |
C-Met mAb (cancer), Eli Lilly; Anti-c-Met antibody (cancer), Lilly
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| External Link | ||||
| SAR-125844 | Phase 2 | [13] | ||
| Synonyms |
Met inhibitor (iv, cancer), sanofi-aventis
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| MOA | Inhibitor | |||
| Activity | IC50 = 4 nM | |||
| External Link | ||||
| Emibetuzumab | Phase 2 | [14] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AMG 337 | Phase 2 | [15] | ||
| MOA | Modulator | |||
| Activity | IC50 = 1 nM | |||
| External Link | ||||
| AMG 208 | Phase 2 | [16] | ||
| Synonyms |
AMG-208; 1002304-34-8; AMG208; UNII-Y2SR66P7VM; 7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline; Y2SR66P7VM; CHEBI:90626; 7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; 7-Methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; C22H17N5O2; 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline; 7-methoxy-4-({6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl}methoxy)quinoline; Triazolopyridazine, 4; 3cd8
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| MOA | Modulator | |||
| Activity | IC50 = 9 nM | |||
| External Link | ||||
| HM-5016504 | Phase 2 | [8] | ||
| Synonyms |
C-Met inhibitor (cancer), Hutchison
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| MOA | Inhibitor | |||
| External Link | ||||
| Telisotuzumab vedotin | Phase 2 | [17] | ||
| Synonyms |
ABBV-399
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| External Link | ||||
| APL-101 | Phase 2 | [18] | ||
| 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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| MOA | Inhibitor | |||
| External Link | ||||
| CMX-2043 | Phase 2 | [19] | ||
| MOA | Modulator | |||
| External Link | ||||
| LY2801653 | Phase 2 | [20] | ||
| Synonyms |
Merestinib; 1206799-15-6; LY-2801653; UNII-5OGS5K699E; N-(3-fluoro-4-((1-methyl-6-(1H-pyrazol-4-yl)-1H-indazol-5-yl)oxy)phenyl)-1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxamide; 5OGS5K699E; N-(3-Fluoro-4-{[1-Methyl-6-(1h-Pyrazol-4-Yl)-1h-Indazol-5-Yl]oxy}phenyl)-1-(4-Fluorophenyl)-6-Methyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide; C30H22F2N6O3; Merestinib [USAN]; SCHEMBL679002; LY2801653 (Merestinib); GTPL9841; CHEMBL3545307; QCR-139; DTXSID20659635; SYN1222; QHADVLVFMKEIIP-UHFFFAOYSA-N
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| MOA | Modulator | |||
| Activity | IC50 = 4.7 nM | |||
| External Link | ||||
| XL880 | Phase 2 | [21] | ||
| Synonyms |
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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| MOA | Modulator | |||
| Activity | IC50 = 0.4 nM | |||
| External Link | ||||
| ChronSeal | Phase 1/2 | [22] | ||
| Synonyms |
Antibiotic-free recombinant HGF, Linkoping; Recombinant HGF, Kringle/ChronTech; Recombinant HGF, Kringle/Tripep
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| MOA | Inhibitor | |||
| External Link | ||||
| Anti-C-met CAR-T cells | Phase 1/2 | [23] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| BMS-777607 | Phase 1/2 | [24] | ||
| Synonyms |
1025720-94-8; BMS 777607; 1196681-44-3; BMS777607; ASLAN-002; UNII-A3MMS6HDO1; N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; A3MMS6HDO1; N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide; N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
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| MOA | Inhibitor | |||
| Activity | IC50 < 2.512 nM | |||
| External Link | ||||
| Sym015 | Phase 1/2 | [9] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| MK-2461 | Phase 1/2 | [25] | ||
| Synonyms |
MK 2461
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.4 nM | |||
| External Link | ||||
| REGN5093 | Phase 1 | [26] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PF-4217903 | Phase 1 | [27] | ||
| Synonyms |
2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol; PF-04217903; 956905-27-4; PF04217903; PF 04217903; UNII-CYJ9ATV1IJ; CYJ9ATV1IJ; CHEMBL2001019; 1159490-85-3; aka PF-04217903; C19H16N8O; 2-[4-(3-Quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-ethanol; 2-(4-(1-(Quinolin-6-ylmethyl)-1H-(1,2,3)triazolo(4,5-b)pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol; 3zxz; PDMUGYOXRHVNMO-UHFFFAOYSA-N
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| MOA | Inhibitor | |||
| Activity | EC50 = 0.3 nM | |||
| External Link | ||||
| ABBV-399 | Phase 1 | [14] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CBT-101 | Phase 1 | [9] | ||
| Synonyms |
L-Asparaginyl-L-leucyl-glycyl-L-valyl-L-[S-(acetamidomethyl)]cysteinamide hydrochloride
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| MOA | Inhibitor | |||
| External Link | ||||
| MK-8033 | Phase 1 | [28] | ||
| Synonyms |
1001917-37-8; UNII-350H6PBQ5Q; 3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-N-(2-pyridinylmethyl)-5H-benzo[4,5]cyclohepta[1,2-b]pyridine-7-methanesulfonamide; 350H6PBQ5Q; CHEMBL2323775; MK8033; 1-(3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo(4,5)cyclohepta(1,2-b)pyridin-7-yl)-N-(pyridin-2-ylmethyl)methanesulfonamide; 1-[2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridin-9-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.6 nM | |||
| External Link | ||||
| Autologous T Cells Expressing MET scFv CAR | Phase 1 | [29] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| ABT-700 | Phase 1 | [30] | ||
| MOA | Modulator | |||
| External Link | ||||
| Hepapoietin | Phase 1 | [31] | ||
| Synonyms |
APS-1010; Hepapoietin, SnowBrand; Hepapoietin (liver/kidney disease); Hepapoietin (liver/kidney disease), Atlas Pharmaceuticals
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| MOA | Inhibitor | |||
| External Link | ||||
| EMD-1204831 | Phase 1 | [32] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| JNJ-38877605 | Phase 1 | [33] | ||
| Synonyms |
C-met inhibitor, Ortho Biotech Oncology Research & Development; C-met inhibitor (solid tumors), ORD/J&J PRD
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.95 nM | |||
| External Link | ||||
| SGX523 | Phase 1 | [34] | ||
| Synonyms |
SGX-523; SGX523, SGX-523
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| MOA | Inhibitor | |||
| Activity | IC50 = 3.1 nM | |||
| External Link | ||||
| TR1801-ADC | Phase 1 | [35] | ||
| External Link | ||||
| LY3164530 | Phase 1 | [36] | ||
| MOA | Modulator | |||
| External Link | ||||
| C-Met/PD-L1 CAR-T Cell | Phase 1 | [37] | ||
| MOA | CAR-T-Cell-Therapy(Dual specific) | |||
| External Link | ||||
| E-7050 | Phase 1 | [38] | ||
| Synonyms |
C-Met and VEGF-2 tyrosine kinase inhibitor (oral, cancer), Eisai
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| MOA | Modulator | |||
| Activity | IC50 = 14 nM | |||
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| XL092 | Phase 1 | [39] | ||
| Synonyms |
SCHEMBL21200856; NSC828252; XL-092; NSC-828252; 2367004-54-2
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| MOA | Inhibitor | |||
| External Link | ||||
| BPI-9016 M | Phase 1 | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AZD9592 | Phase 1 | [41] | ||
| External Link | ||||
| TPX-0022 | Phase 1 | [42] | ||
| Synonyms |
CSF1R-IN-2; SCHEMBL20694441; TPX0022; NSC820832; NSC-820832; HY-111787; CS-0091874; 2271119-26-5
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| MOA | Inhibitor | |||
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| RXDX-106 | Phase 1 | [43] | ||
| Synonyms |
CEP-40783; 1437321-24-8; CEP40783; UNII-1969ZJE05Q; 1969ZJE05Q; N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1-isopropyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide; N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-3-(4-fluorophenyl)-2,4-dioxo-1-propan-2-ylpyrimidine-5-carboxamide; RXDX-106 (CEP-40783); SCHEMBL16089863; BCP25839; EX-A2540; MFCD28502441; NSC797770; s8570; AKOS032960472; ZINC205893112; CCG-270157; CS-6371; NSC-797770; SB18930; AC-31425; AS-35141; HY-100946; N-(4-((6,7-Dimethoxy-4-quinolinyl)oxy)-3-fluorophenyl)-3-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-(1-methylethyl)-2,4-dioxo-5-pyrimidinecarboxamide
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| MOA | Inhibitor | |||
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| Altiratinib | Phase 1 | [44] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2.7 nM | |||
| External Link | ||||
| Mteron-F1 | Preclinical | [45] | ||
| MOA | Stimulator | |||
| External Link | ||||
| NPS-1034 | Preclinical | [46] | ||
| Synonyms |
1221713-92-3; CHEMBL3810063; 1-(4-fluorophenyl)-N-[3-fluoro-4-[(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,3-dimethyl-5-oxopyrazole-4-carboxamide; N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide.; SCHEMBL1963111; BCP15998; NPS1034;NPS 1034; BDBM50172077; s7669; ZINC68204845; CCG-270007; NCGC00481564-01; AC-31427; AK685795; BS-14709; HY-100509; CS-0019643; N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide; S4K
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| MOA | Inhibitor | |||
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| ALD-805 | Investigative | [8] | ||
| External Link | ||||
| PHA-665752 | Investigative | [8] | ||
| Synonyms |
477575-56-7; PHA 665752; PHA665752; TCMDC-125885; UNII-0VXU5T5R3J; (2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE; 0VXU5T5R3J; CHEMBL450786; CHEBI:90197; (R,Z)-5-(2,6-dichlorobenzylsulfonyl)-3-((3,5-dimethyl-4-(2-(pyrrolidin-1-ylmethyl)pyrrolidine-1-carbonyl)-1H-pyrrol-2-yl)methylene)indolin-2-one; PHA-665752 hydrate
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| MOA | Inhibitor | |||
| Activity | IC50 = 9 nM | |||
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| APS-3010 | Investigative | [8] | ||
| Synonyms |
Hepatic growth factor inhibitor (cancer), Atlas Pharmaceuticals
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| MOA | Inhibitor | |||
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| LA-480 | Investigative | [8] | ||
| Synonyms |
Bispecific c-Met monoclonal antibody (cancer), Lilly
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| External Link | ||||
| Anti-cMET mab | Investigative | [8] | ||
| Synonyms |
Anti-cMET mAb (undisclosed indication); Anti-cMET mAb (undisclosed indication), PharmAbcine; CMET inhibitor (mAb, undisclosed indication), PharmAbcine
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| MOA | Inhibitor | |||
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| AM7 | Investigative | [47] | ||
| Synonyms |
pyrimidone, 22; AM 7; AM-7
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| MOA | Inhibitor | |||
| Activity | IC50 = 8.9 nM | |||
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| mab 224G11 | Investigative | [8] | ||
| Synonyms |
C-Met antagonist monoclonal antibody (cancer); C-Met antagonist monoclonal antibody (cancer), Pierre Fabre/Abbott
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| TP-801 | Investigative | [8] | ||
| Synonyms |
C-Met tyrosine kinase inhibitor (oral, cancer), Tiger Pharmatech
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| MOA | Inhibitor | |||
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| SU11274 | Investigative | [48] | ||
| Synonyms |
Met kinase Inhibitor; SU-11274
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
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| PF-00614435 | Investigative | [8] | ||
| Synonyms |
PF-00658968; PF-00851623; PF-02311803; PF-4254644; PF-851623; PF-899555; C-Met (HGFR) inhibitors (cancer), Pfizer
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| MOA | Inhibitor | |||
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| CMET Avimer polypeptides | Investigative | [8] | ||
| Synonyms |
CMET Avimer polypeptides (cancer); MEDI-555; CMET Avimer polypeptides (cancer), MedImmmue; CMET-targeting anticancer avimers, MedImmune; CMET-targeting avimers (cancer), Avidia/MedImmune
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| MOA | Inhibitor | |||
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| PRS-110 | Investigative | [8] | ||
| Synonyms |
C-Met inhibitor (cancer), Pieris; C-mesenchymal-epithelial transition factor (lipoprotein/protein recombinant, cancer), Pieris AG
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| MOA | Inhibitor | |||
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| 1-benzyl-1H-pyrrolo[3,2-b]pyridine | Investigative | [49] | ||
| Synonyms |
CHEMBL561256; 1-benzyl-4-azaindole; 1h-pyrrolo[3,2-b]pyridine,1-(phenylmethyl)-; SCHEMBL4716978; LOGFFHFLSCMKJF-UHFFFAOYSA-N; BDBM50295764; ZINC43079815; 50426-35-2
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| MOA | Inhibitor | |||
| Activity | IC50 = 19 nM | |||
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| RP-1040 | Investigative | [8] | ||
| Synonyms |
RP-1086; RP-1087; RP-1088; RP-1101; RP-1103; RP-1105; RP-1109; RP-1110; RP-1111; RP-1112; C-Met kinase inhibitors (oral,cancer); C-Met kinase inhibitors (oral, cancer), Incozen Therapeutics/Rhizen Pharmaceuticals
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| MOA | Inhibitor | |||
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| BAY-85-3474 | Investigative | [8] | ||
| Synonyms |
Met inhibitor (cancer), Bayer Schering
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| MOA | Inhibitor | |||
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| GE-137 | Investigative | [50] | ||
| MOA | Modulator | |||
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| 3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine | Investigative | [49] | ||
| Synonyms |
CHEMBL538932; 633303-90-9; SCHEMBL3889418; CTK2A9458; DTXSID00621754; XIVJYIWQYBHEBJ-UHFFFAOYSA-N; BDBM50295740; 3-(Benzenesulfonyl)-1H-pyrrolo[2,3-b]pyridine; 1H-Pyrrolo[2,3-b]pyridine, 3-(phenylsulfonyl)-
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| MOA | Inhibitor | |||
| Activity | IC50 = 1175 nM | |||
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| 1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine | Investigative | [49] | ||
| Synonyms |
CHEMBL540744
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| MOA | Inhibitor | |||
| Activity | IC50 = 250 nM | |||
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| ALD-806 | Investigative | [8] | ||
| Synonyms |
Anti-HGF mAb (cancer), Alder Biopharmaceuticals
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| 1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine | Investigative | [49] | ||
| Synonyms |
1-(Phenylsulfonyl)-4-azaindole; 677302-44-2; CHEMBL556118; SCHEMBL3705420; HGOGRVVSSAWHTO-UHFFFAOYSA-N; BDBM50295729; ZINC42923799; AKOS032961360; KB-3354225
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| MOA | Inhibitor | |||
| Activity | IC50 = 3500 nM | |||
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| DP-3590 | Investigative | [8] | ||
| Synonyms |
DP-4157; DP-4693; DP-4756; C-Met kinase inhibitors (solid tumor/metastatic cancer); C-Met kinase inhibitors (solid tumor/metastatic cancer), Deciphera
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| MOA | Inhibitor | |||
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| HuMax-cMet | Investigative | [8] | ||
| Synonyms |
CMet-targeting human IgG1 antibody (cancer), Genmab
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| YH013 | Investigative | [51] | ||
| External Link | ||||
| PMID24210504C1o | Investigative | [52] | ||
| Synonyms |
GTPL8143; BDBM50444090
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| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
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| PMID21123062C27 | Investigative | [53] | ||
| Synonyms |
GTPL8210; BDBM50334085
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| MOA | Inhibitor | |||
| Activity | IC50 = 44 nM | |||
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| PMID21967808CR-16 | Investigative | [54] | ||
| Synonyms |
GTPL8213; BDBM50361564
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM | |||
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| BMS-536924 | Investigative | [55] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 4870 nM | |||
| External Link | ||||
| 2C25: Lung cancer | 52 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Adagrasib | Approved | [56] | ||
| 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 | [57] | ||
| External Link | ||||
| Mobocertinib | Approved | [58] | ||
| 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 | [59] | ||
| External Link | ||||
| Sacituzumab govitecan | Approved | [60] | ||
| 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 | [61] | ||
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| Tepotinib | Approved | [4] | ||
| 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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| Sotorasib | Approved | [62] | ||
| 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 | [63] | ||
| 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 | [64] | ||
| Synonyms |
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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| MYL-1402O | Phase 3 | [65] | ||
| Synonyms |
bevacizumab biosimilar
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| AB154 | Phase 3 | [66] | ||
| Synonyms |
Domvanalimab
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| Datopotamab deruxtecan | Phase 3 | [67] | ||
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| CS1001 | Phase 3 | [68] | ||
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| JDQ443 | Phase 3 | [69] | ||
| 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 | [70] | ||
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| Tusamitamab ravtansine | Phase 3 | [71] | ||
| Synonyms |
SAR408701
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| RG6058 | Phase 3 | [72] | ||
| Synonyms |
Tiragolumab
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| GSK4069889 | Phase 2 | [73] | ||
| Synonyms |
TSR-022
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| APL-101 | Phase 2 | [74] | ||
| 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 | [75] | ||
| Synonyms |
Ladiratuzumab Vedotin
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| BNT116 | Phase 2 | [76] | ||
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| AZD7789 | Phase 2 | [77] | ||
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| L-DOS47 | Phase 1/2 | [78] | ||
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| NC318 | Phase 2 | [79] | ||
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| Vorolanib | Phase 2 | [80] | ||
| Synonyms |
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 | [81] | ||
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| Bintrafusp alfa | Phase 2 | [82] | ||
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| Voyager-V1 | Phase 2 | [83] | ||
| Synonyms |
VSV-IFNBeta-NIS
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| AB-106 | Phase 2 | [84] | ||
| Synonyms |
DS6051b; GTPL11198; AB106
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| RO-5126766 | Phase 2 | [85] | ||
| Synonyms |
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TC-210 | Phase 1/2 | [86] | ||
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| EMB-01 | Phase 1/2 | [87] | ||
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| NM21-1480 | Phase 1/2 | [88] | ||
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| MRx0518 | Phase 1/2 | [89] | ||
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| DZD9008 | Phase 1/2 | [90] | ||
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| BGB-A425 | Phase 1/2 | [91] | ||
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| Rilvegostomig | Phase 1/2 | [92] | ||
| Synonyms |
AZD2936
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| IK-007 | Phase 1/2 | [93] | ||
| Synonyms |
grapiprant
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| IBI318 | Phase 1 | [94] | ||
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| GEN-011 | Phase 1 | [95] | ||
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| ENV-105 | Phase 1 | [96] | ||
| Synonyms |
Carotuximab
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| AMG 160 | Phase 1 | [97] | ||
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| ADP-A2M10 | Phase 1 | [98] | ||
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| MEDI5752 | Phase 1 | [99] | ||
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| PF-07104091 | Phase 1 | [100] | ||
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| PF-06936308 | Phase 1 | [101] | ||
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| GEM3PSCA | Phase 1 | [102] | ||
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| PF-07257876 | Phase 1 | [103] | ||
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| Cosibelimab | Phase 1 | [104] | ||
| Synonyms |
CK-301/TG-1501
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| Gemcitabine | Approved | [7] | ||
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| SMI-4a | Investigative | [105] | ||
| 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