OSI-930

SKU: orb1224130

Description

A potent, orally active, dual inhibitor of c-Kit and VEGFR-2 (KDR) with IC50 of 15 nM and 9 nM, respectively; also inhibits Lck, c-Raf, Flt1, and CSF-1R (IC50<100 nM); exhibits antitumor activity in mutant Kit-expressing HMC-1 xenograft model.Solid Tumors Phase 1 Discontinued(In Vitro):OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase. OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM. OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner.(In Vivo):OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models.

Key Properties

• CAS Number: 728033-96-3
• MW: 443.4416
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₆F₃N₃O₂S
• SMILES: O=C(C1=C(NCC2=CC=NC3=CC=CC=C23)C=CS1)NC4=CC=C(OC(F)(F)F)C=C4
• Target: c-Kit
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models. Animal model: Female nu/nu CD-1 mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models. Dosage: 200 mg/kg. Administration: Oral gavage; once a day; 38 days. Result: Showed a significant level of inhibition of Kit, KDR and CSF-1R.
• In Vitro:
  OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase. OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM. OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OSI 930 | OSI930

Quick Database Links

Gene Symbol

c-Kit