OSI-930 Chemical Structure
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
Dovitinib(TKI-258) is a highly potent, novel multitargeted growth factor receptor kinase inhibitor with IC50 of 1, 2, 5, 10, 8, 27, 36 nM for FLT3, c-KIT, FGFR, VEGFR1/2/3, PDGFRß and CSF-1R, respectively.
Dasatinib also known as BMS-354825, Sprycel, BMS354825 is ATP-competitive, dual SRC/ABL inhibitor. BMS-354825 inhibits all members of the Src family, including c-Src, Lck, Fyn, and Yes (IC50 < 1.1nmol/L).
Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 μM for the inhibition of T-cell proliferation stimulated by DCs and PHA, respectively.
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors
Pazopanib HCl is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.
Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
OSI-930 is a multi-targeted tyrosine kinase inhibitor that is designed to act as a potent co-inhibitor of the receptor tyrosine kinases c-Kit (IC50:9.5nM) and VEGFR-2 (IC50:10.1nM). [1]
OSI-930 targets both cancer cell proliferation and blood vessel growth (angiogenesis) in selected tumors. In preclinical studies, OSI-930 shows broad efficacy in tumor models representative of small cell lung cancer, glioblastoma, colorectal, renal, head and neck, non-small cell lung cancer and gastric cancers. [1]
| Molecular Weight (WM): | 443.44 |
|---|---|
| Formula: | C22H16F3N3O2S |
| CAS No.: | 728033-96-3 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥89mg/mL |
| Water <1mg/mL | |
| Ethanol ≥6mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
A collection of 426 FDA approved drugs
A collection of 139 natural products
A collection of 40 chemotherapeutic agents
A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of OSI-930 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan |
For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of OSI-930 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan
Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center.OSI-930 purchased from Selleck OSI-930 purchased from Selleck
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