| Stereochemistry | ABSOLUTE |
| Molecular Formula | C23H19N3O2 |
| Molecular Weight | 369.4159 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C1NC(=O)[C@H]([C@@H]1C2=CNC3=C2C=CC=C3)C4=CN5CCCC6=CC=CC4=C56
InChI
InChIKey=UCEQXRCJXIVODC-PMACEKPBSA-N
InChI=1S/C23H19N3O2/c27-22-19(16-11-24-18-9-2-1-7-14(16)18)20(23(28)25-22)17-12-26-10-4-6-13-5-3-8-15(17)21(13)26/h1-3,5,7-9,11-12,19-20,24H,4,6,10H2,(H,25,27,28)/t19-,20-/m0/s1
| Molecular Formula | C23H19N3O2 |
| Molecular Weight | 369.4159 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Tivantinib (ARQ 197) is the first non-ATP-competitive small molecule that selectively targets the c-Met receptor tyrosine kinase. Exposure to Tivantinib resulted in the inhibition of proliferation of c-Met-expressing cancer cell lines as well as the induction of caspase-dependent apoptosis in cell lines with constitutive c-Met activity. ArQule and its collaborators Daiichi Sankyo and Kyowa Hakko Kirin are developing tivantinib as a potential therapy for many cancers. c-Met is overexpressed in many cancers. Tivantinib currently is in phase 3 clinical development for the treatment of hepatocellular carcinoma and non-small cell lung cancer.
Originator
Approval Year
Sourcing
PubMed
Sample Use Guides
The initially identified dose and schedule for clinical use (hepatocellular carcinoma treatment) was 360 mg twice daily. During study conduction, tivantinib dose was amended to 240 mg twice daily, due to a high incidence of neutropenia, without losing clinical efficacy.
Route of Administration:
Oral
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TARGET -> INHIBITOR |
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