OSI-930

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity[1].

Product Specifications

CAS Number

[728033-96-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; c-Fms; c-Kit; VEGFR

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/OSI-930.html

Purity

99.01

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=C(NCC2=CC=NC3=CC=CC=C23)C=CS1)NC4=CC=C(OC(F)(F)F)C=C4

Molecular Formula

C22H16F3N3O2S

Molecular Weight

443.44

Precautions

H302, H315, H319, H335

References & Citations

[1]Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66 (2) :1015-1024.|[2]Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39 (2), 345-350.