m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT02172
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[1], [2] | |||
DNA methylation
DNMT3A
METTL3
Direct
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 | DNA methylation (DNAMeth) | ||||
| Epigenetic Regulator | Cysteine methyltransferase DNMT3A (DNMT3A) | WRITER | View Details | ||
| Regulated Target | Methyltransferase-like protein 3 (METTL3) | View Details | |||
| Crosstalk Relationship | DNA methylation → m6A | Inhibition | |||
| Crosstalk Mechanism | DNA methylation directly impacts m6A modification through modulating the expression level of m6A regulator | ||||
| Crosstalk Summary | Methyltransferase-like 3 (METTL3) increased the pri-Let-7b, decreased both the pre-Let-7b and mature Let-7b, attenuating the Let-7b controlling of stem cell renewal. The addition of Metformin increased the bindings of DNA methyltransferase-3a/b (DNMT3A/DNMT3B) to the METTL3 promoter. With the help of the readers of NKAP and HNRNPA2B1, the cluster mediated m6A formation on pri-Let-7b processing increased the mature Let-7b, the key player in suppressing Notch signaling and re-captivating Osimertinib treatment. 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 | Osimertinib | ||||
| Pathway Response | PI3K-Akt signaling pathway | hsa04151 | |||
| Cell Process | Cell proliferation | ||||
In-vitro Model |
NCI-H1975 | Lung adenocarcinoma | Homo sapiens | CVCL_1511 | |
| HCC827 | Lung adenocarcinoma | Homo sapiens | CVCL_2063 | ||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Cysteine methyltransferase DNMT3A (DNMT3A) | 8 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| PMID27376512-Compound-Figure3CN | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CG | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 2400 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure3CM | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | EC50 = 1100 nM | |||
| External Link | ||||
| PMID27376512-Compound-Figure2aExample1 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 3000 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-424 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1940 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-427 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 295 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-422 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1430 nM | |||
| External Link | ||||
| PMID27376512-Compound-MTC-423 | Patented | [3] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 363 nM | |||
| External Link | ||||
| Hepatocyte growth factor receptor (c-Met/MET) | 76 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Capmatinib | Approved | [4] | ||
| 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 | [5] | ||
| 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 | [6] | ||
| Synonyms |
Cabometyx; Cometriq
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| MOA | Inhibitor | |||
| Activity | IC50 = 1.3 nM | |||
| External Link | ||||
| Amivantamab | Approved | [7] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Crizotinib | Approved | [8] | ||
| Synonyms |
Xalkori (TN); novel ALK inhibitors
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| MOA | Modulator | |||
| Activity | IC50 = 0.51 nM | |||
| External Link | ||||
| RG3638 | Phase 3 | [9] | ||
| Synonyms |
Onartuzumab
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| MOA | Modulator | |||
| External Link | ||||
| Savolitinib | Phase 3 | [10] | ||
| 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 | [11] | ||
| MOA | Modulator | |||
| External Link | ||||
| Tivantinib | Phase 3 | [12] | ||
| 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 | [9] | ||
| Synonyms |
Sitravatinib
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| MOA | Inhibitor | |||
| External Link | ||||
| LY-2875358 | Phase 2 | [13] | ||
| Synonyms |
C-Met mAb (cancer), Eli Lilly; Anti-c-Met antibody (cancer), Lilly
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| External Link | ||||
| SAR-125844 | Phase 2 | [14] | ||
| Synonyms |
Met inhibitor (iv, cancer), sanofi-aventis
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| MOA | Inhibitor | |||
| Activity | IC50 = 4 nM | |||
| External Link | ||||
| Emibetuzumab | Phase 2 | [15] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AMG 337 | Phase 2 | [16] | ||
| MOA | Modulator | |||
| Activity | IC50 = 1 nM | |||
| External Link | ||||
| AMG 208 | Phase 2 | [17] | ||
| 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 | [9] | ||
| Synonyms |
C-Met inhibitor (cancer), Hutchison
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| MOA | Inhibitor | |||
| External Link | ||||
| Telisotuzumab vedotin | Phase 2 | [18] | ||
| Synonyms |
ABBV-399
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| External Link | ||||
| APL-101 | Phase 2 | [19] | ||
| 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 | [20] | ||
| MOA | Modulator | |||
| External Link | ||||
| LY2801653 | Phase 2 | [21] | ||
| 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 | [22] | ||
| 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 | [23] | ||
| 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 | [24] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| BMS-777607 | Phase 1/2 | [25] | ||
| 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 | [10] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| MK-2461 | Phase 1/2 | [26] | ||
| Synonyms |
MK 2461
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| MOA | Inhibitor | |||
| Activity | IC50 = 0.4 nM | |||
| External Link | ||||
| REGN5093 | Phase 1 | [27] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PF-4217903 | Phase 1 | [28] | ||
| 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 | [15] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CBT-101 | Phase 1 | [10] | ||
| 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 | [29] | ||
| 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 | [30] | ||
| MOA | CAR-T-Cell-Therapy | |||
| External Link | ||||
| ABT-700 | Phase 1 | [31] | ||
| MOA | Modulator | |||
| External Link | ||||
| Hepapoietin | Phase 1 | [32] | ||
| 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 | [33] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| JNJ-38877605 | Phase 1 | [34] | ||
| 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 | [35] | ||
| Synonyms |
SGX-523; SGX523, SGX-523
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| MOA | Inhibitor | |||
| Activity | IC50 = 3.1 nM | |||
| External Link | ||||
| TR1801-ADC | Phase 1 | [36] | ||
| External Link | ||||
| LY3164530 | Phase 1 | [37] | ||
| MOA | Modulator | |||
| External Link | ||||
| C-Met/PD-L1 CAR-T Cell | Phase 1 | [38] | ||
| MOA | CAR-T-Cell-Therapy(Dual specific) | |||
| External Link | ||||
| E-7050 | Phase 1 | [39] | ||
| 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 | [40] | ||
| Synonyms |
SCHEMBL21200856; NSC828252; XL-092; NSC-828252; 2367004-54-2
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| MOA | Inhibitor | |||
| External Link | ||||
| BPI-9016 M | Phase 1 | [41] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AZD9592 | Phase 1 | [42] | ||
| External Link | ||||
| TPX-0022 | Phase 1 | [43] | ||
| Synonyms |
CSF1R-IN-2; SCHEMBL20694441; TPX0022; NSC820832; NSC-820832; HY-111787; CS-0091874; 2271119-26-5
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| MOA | Inhibitor | |||
| External Link | ||||
| RXDX-106 | Phase 1 | [44] | ||
| 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 | [45] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2.7 nM | |||
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| Mteron-F1 | Preclinical | [46] | ||
| MOA | Stimulator | |||
| External Link | ||||
| NPS-1034 | Preclinical | [47] | ||
| 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 | [9] | ||
| External Link | ||||
| PHA-665752 | Investigative | [9] | ||
| 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 | [9] | ||
| Synonyms |
Hepatic growth factor inhibitor (cancer), Atlas Pharmaceuticals
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| MOA | Inhibitor | |||
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| LA-480 | Investigative | [9] | ||
| Synonyms |
Bispecific c-Met monoclonal antibody (cancer), Lilly
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| Anti-cMET mab | Investigative | [9] | ||
| 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 | [48] | ||
| 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 | [9] | ||
| Synonyms |
C-Met antagonist monoclonal antibody (cancer); C-Met antagonist monoclonal antibody (cancer), Pierre Fabre/Abbott
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| TP-801 | Investigative | [9] | ||
| Synonyms |
C-Met tyrosine kinase inhibitor (oral, cancer), Tiger Pharmatech
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| MOA | Inhibitor | |||
| External Link | ||||
| SU11274 | Investigative | [49] | ||
| Synonyms |
Met kinase Inhibitor; SU-11274
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| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
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| PF-00614435 | Investigative | [9] | ||
| 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 | |||
| External Link | ||||
| CMET Avimer polypeptides | Investigative | [9] | ||
| 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 | |||
| External Link | ||||
| PRS-110 | Investigative | [9] | ||
| Synonyms |
C-Met inhibitor (cancer), Pieris; C-mesenchymal-epithelial transition factor (lipoprotein/protein recombinant, cancer), Pieris AG
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| MOA | Inhibitor | |||
| External Link | ||||
| 1-benzyl-1H-pyrrolo[3,2-b]pyridine | Investigative | [50] | ||
| 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 | [9] | ||
| 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 | |||
| External Link | ||||
| BAY-85-3474 | Investigative | [9] | ||
| Synonyms |
Met inhibitor (cancer), Bayer Schering
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| MOA | Inhibitor | |||
| External Link | ||||
| GE-137 | Investigative | [51] | ||
| MOA | Modulator | |||
| External Link | ||||
| 3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine | Investigative | [50] | ||
| 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 | [50] | ||
| Synonyms |
CHEMBL540744
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| MOA | Inhibitor | |||
| Activity | IC50 = 250 nM | |||
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| ALD-806 | Investigative | [9] | ||
| Synonyms |
Anti-HGF mAb (cancer), Alder Biopharmaceuticals
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| 1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine | Investigative | [50] | ||
| 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 | [9] | ||
| 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 | |||
| External Link | ||||
| HuMax-cMet | Investigative | [9] | ||
| Synonyms |
CMet-targeting human IgG1 antibody (cancer), Genmab
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| External Link | ||||
| YH013 | Investigative | [52] | ||
| External Link | ||||
| PMID24210504C1o | Investigative | [53] | ||
| Synonyms |
GTPL8143; BDBM50444090
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| MOA | Inhibitor | |||
| Activity | IC50 = 8 nM | |||
| External Link | ||||
| PMID21123062C27 | Investigative | [54] | ||
| Synonyms |
GTPL8210; BDBM50334085
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| MOA | Inhibitor | |||
| Activity | IC50 = 44 nM | |||
| External Link | ||||
| PMID21967808CR-16 | Investigative | [55] | ||
| Synonyms |
GTPL8213; BDBM50361564
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| MOA | Inhibitor | |||
| Activity | IC50 = 26 nM | |||
| External Link | ||||
| BMS-536924 | Investigative | [56] | ||
| 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 | [57] | ||
| 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 | [58] | ||
| External Link | ||||
| Mobocertinib | Approved | [59] | ||
| 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 | [60] | ||
| External Link | ||||
| Sacituzumab govitecan | Approved | [61] | ||
| 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 | [62] | ||
| External Link | ||||
| Tepotinib | Approved | [5] | ||
| 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 | [63] | ||
| 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 | [64] | ||
| 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 | [65] | ||
| Synonyms |
FIKPXCOQUIZNHB-RRKGBCIJSA-N; SCHEMBL20438940; TPX 0005; BCP19778
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| MYL-1402O | Phase 3 | [66] | ||
| Synonyms |
bevacizumab biosimilar
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| AB154 | Phase 3 | [67] | ||
| Synonyms |
Domvanalimab
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| Datopotamab deruxtecan | Phase 3 | [68] | ||
| External Link | ||||
| CS1001 | Phase 3 | [69] | ||
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| JDQ443 | Phase 3 | [70] | ||
| 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 | [71] | ||
| External Link | ||||
| Tusamitamab ravtansine | Phase 3 | [72] | ||
| Synonyms |
SAR408701
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| RG6058 | Phase 3 | [73] | ||
| Synonyms |
Tiragolumab
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| GSK4069889 | Phase 2 | [74] | ||
| Synonyms |
TSR-022
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| APL-101 | Phase 2 | [75] | ||
| 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 | [76] | ||
| Synonyms |
Ladiratuzumab Vedotin
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| BNT116 | Phase 2 | [77] | ||
| External Link | ||||
| AZD7789 | Phase 2 | [78] | ||
| External Link | ||||
| L-DOS47 | Phase 1/2 | [79] | ||
| External Link | ||||
| NC318 | Phase 2 | [80] | ||
| External Link | ||||
| Vorolanib | Phase 2 | [81] | ||
| 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 | [82] | ||
| External Link | ||||
| Bintrafusp alfa | Phase 2 | [83] | ||
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| Voyager-V1 | Phase 2 | [84] | ||
| Synonyms |
VSV-IFNBeta-NIS
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| AB-106 | Phase 2 | [85] | ||
| Synonyms |
DS6051b; GTPL11198; AB106
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| RO-5126766 | Phase 2 | [86] | ||
| Synonyms |
VS-6766; CH-5126766; Dual Raf/MEK protein kinase inhibitor (cancer), Roche
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| TC-210 | Phase 1/2 | [87] | ||
| External Link | ||||
| EMB-01 | Phase 1/2 | [88] | ||
| External Link | ||||
| NM21-1480 | Phase 1/2 | [89] | ||
| External Link | ||||
| MRx0518 | Phase 1/2 | [90] | ||
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| DZD9008 | Phase 1/2 | [91] | ||
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| BGB-A425 | Phase 1/2 | [92] | ||
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| Rilvegostomig | Phase 1/2 | [93] | ||
| Synonyms |
AZD2936
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| IK-007 | Phase 1/2 | [94] | ||
| Synonyms |
grapiprant
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| IBI318 | Phase 1 | [95] | ||
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| GEN-011 | Phase 1 | [96] | ||
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| ENV-105 | Phase 1 | [97] | ||
| Synonyms |
Carotuximab
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| AMG 160 | Phase 1 | [98] | ||
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| ADP-A2M10 | Phase 1 | [99] | ||
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| MEDI5752 | Phase 1 | [100] | ||
| External Link | ||||
| PF-07104091 | Phase 1 | [101] | ||
| External Link | ||||
| PF-06936308 | Phase 1 | [102] | ||
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| GEM3PSCA | Phase 1 | [103] | ||
| External Link | ||||
| PF-07257876 | Phase 1 | [104] | ||
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| Cosibelimab | Phase 1 | [105] | ||
| Synonyms |
CK-301/TG-1501
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| Gemcitabine | Approved | [8] | ||
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| SMI-4a | Investigative | [106] | ||
| 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