| Stereochemistry | ACHIRAL |
| Molecular Formula | C22H16F3N3O2S |
| Molecular Weight | 443.442 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)OC1=CC=C(NC(=O)C2=C(NCC3=CC=NC4=CC=CC=C34)C=CS2)C=C1
InChI
InChIKey=FGTCROZDHDSNIO-UHFFFAOYSA-N
InChI=1S/C22H16F3N3O2S/c23-22(24,25)30-16-7-5-15(6-8-16)28-21(29)20-19(10-12-31-20)27-13-14-9-11-26-18-4-2-1-3-17(14)18/h1-12,27H,13H2,(H,28,29)
| Molecular Formula | C22H16F3N3O2S |
| Molecular Weight | 443.442 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
OSI-930 (now SIM-930) is a potent, oral small-molecule receptor tyrosine kinase inhibitor, which acts predominantly against VEGF receptors (VEGFR), c-Kit, and platelet-derived growth factor receptors. OSI-930 has a pharmacokinetic-pharmacodynamic profile distinct from other RTK inhibitors, with potent antitumor activity in multiple xenograft models. OSI-930 passed through phase I clinical trial in the USA (in patients with advanced solid tumors) and recieved the clinical approval by China FDA after being out-licensed to Simcere Pharma in China.
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
The maximum-tolerated dose is 500 mg given twice a day.
Route of Administration:
Oral
HMC-1 mast cell leukemia cells, COLO 205, and aortic rings were incubated with OSI-930 (10, 100, and 1000 nM) for 24h (apoptosis-caspase 3/7 activity), 48h (cell viability), or 10d (endothelial sprout formation). For HMC-1 cells IC50 value were 14 and 34 nM in cell viability and apoptosis assay, respectively.
