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OSI-930

Catalog No. T2624   CAS 728033-96-3
Synonyms: OSI 930

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
OSI-930 Chemical Structure
OSI-930, CAS 728033-96-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 47.00
2 mg In stock $ 66.00
5 mg In stock $ 103.00
10 mg In stock $ 175.00
25 mg In stock $ 339.00
50 mg In stock $ 576.00
100 mg In stock $ 825.00
1 mL * 10 mM (in DMSO) In stock $ 103.00
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Purity: 99.76%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
Targets&IC50 Flt1:8 nM, CSF-1R:15 nM, KDR:9 nM, C-Raf:41 nM, Lck:22 nM
Kinase Assay Protein kinase assays : Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at ?80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit.
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)
Synonyms OSI 930
Molecular Weight 443.44
Formula C22H16F3N3O2S
CAS No. 728033-96-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 82 mg/mL (184.9 mM)

Ethanol: 3 mg/mL (6.76 mM)

TargetMolReferences and Literature

1. Garton AJ, et al. Cancer Res. 2006, 66(2):1015-1024. 2. Lin HL, et al. Drug Metab Dispos. 2011, 39(2), 345-350. 3. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969.

TargetMolCitations

1. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cardiovascular Disease Compound Library Cytokine Inhibitor Library Immuno-Oncology Compound Library Kinase Inhibitor Library Anti-Liver Cancer Compound Library Anti-Colorectal Cancer Compound Library

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Keywords

OSI-930 728033-96-3 Angiogenesis Apoptosis MAPK Tyrosine Kinase/Adaptors c-Fms Raf VEGFR FLT c-Kit Src CSF-1R Inhibitor CD117 Vascular endothelial growth factor receptor CSF1R colony stimulating factor 1 receptor antitumor OSI 930 SCFR selective OSI930 CSF-1 receptor inhibit inhibitor

 

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