OSI-930

SKU: orb1305252

Description

OSI-930 is an orally bioavailable small molecule dual inhibitor of c-Kit and VEGFR-2 tyrosine kinases. It is used in cancer research to study mechanisms of tumor cell proliferation and angiogenesis, with applications in both in vitro assays and in vivo xenograft models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 728033-96-3
• MW: 443.44
• Purity: 99.67% (May vary between batches)
• Formula: C₂₂H₁₆F₃N₃O₂S
• SMILES: FC(F)(F)Oc1ccc(NC(=O)c2sccc2NCc2ccnc3ccccc23)cc1
• Target: Src,FLT,CSF-1R,VEGFR,Apoptosis,c-Fms,c-Kit,Raf
• Solubility: DMSO:82 mg/mL (184.92 mM);Ethanol:3 mg/mL (6.77 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.44 mM)

Bioactivity

• Target IC50:
  Abl:4738 nM|CSF1R:15 nM|KDR:9 nM|c-Kit:80 nM|PDGFRα:3408 nM|PDGFRβ:6900 nM|FLT3:1303 nM|C-Raf:41 nM|Lck:22 nM|FLK1:8 nM
• In Vivo:
  In HMC-1 cell line (IC50=14 nM), OSI-930 inhibited cell proliferation and induced apoptosis.OSI-930 was able to inhibit a variety of recombinant receptor tyrosine kinases, Kit (IC50=80 nM), KDR (IC50=9 nM), Flt (IC50=8 nM), CSF-1R (IC50=15 nM), c- Raf (IC50=41 nM) and Lck (IC50=22 nM).
• In Vitro:
  In HMC-1 cell line (IC50=14 nM), OSI-930 inhibited cell proliferation and induced apoptosis.OSI-930 was able to inhibit a variety of recombinant receptor tyrosine kinases, Kit (IC50=80 nM), KDR (IC50=9 nM), Flt (IC50=8 nM), CSF-1R (IC50=15 nM), c- Raf (IC50=41 nM) and Lck (IC50=22 nM).
• Cell Research:
  For assays of cell proliferation and apoptosis, cells are seeded into 96-well plates and incubated for 2 to 3 days in the presence of OSI-930 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of the intracellular ATP content using CellTiterGlo. Induction of caspase-dependent apoptosis by OSI-930 is quantitated by an enzymatic caspase 3/7 assay. Inhibition of angiogenesis by OSI-930 is monitored using the rat aortic ring endothelial sprout outgrowth assay. Sections of aorta are prepared from CO2-euthanized male rats and cultured in vitro in a collagen matrix in the presence or absence of OSI-930. The collagen matrix is prepared from type 1 rat tail collagen solubilized in 0.1% acetic acid at 3 mg/mL, which is combined with 0.125 volume collagen buffer (0.05 N NaOH, 200 mM HEPES, 260 mM NaHCO3), 0.125 volume of medium 199, 0.0125 volume of 1 M NaOH, and 1% GlutaMax. Aortic rings are embedded in 0.4 mL of this matrix in six-well plates, to which 0.5 mL endothelial basal medium and the appropriate amount of OSI-930 is added; the rings are then incubated for 10 days and the resultant angiogenic sprout outgrowth is digitally quantitated from images by measurement of the sprout-containing area within a series of concentric rings around the aortic tissue area.(Only for Reference)

Storage & Handling

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

Alternative Names

Apoptosis, antitumor, C-Raf, CSF-1 receptor, CSF1R, CSF-1R, colony stimulating factor 1 receptor, cKit, c-Kit, cFms, c-Fms, CD117, OSI 930, OSI930, OSI-930, inhibit, Inhibitor, Lck, FLT1, selective, SCFR, Vascular endothelial growth factor receptor, VEGFR, VEGFR2 (KDR)

Compound Identifiers

PubChem CID

9868037