OSI-930

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OSI-930

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Cat No: 29379

Biochemicals - Kinase Inhibitors

OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

3-[(4-quinolinylmethyl)amino]-N-[4-(trifluoromethoxy)phenyl]-2-thiophenecarboxamide

Correlated keywords:

FLT 1 HMC1 NCIH526 OSI930 VEGFR 2 CSF 1R V560 G

Product Overview:
OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM).{52291} It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8, 15, 41, and 22 nM, respectively). OSI-930 inhibits Kit autophosphorylation in NCI-H526 and HMC-1 cells expressing wild-type Kit and Kit containing the constitutively active V560G mutation (KitV560G), respectively, and stem cell factor-induced Kit autophosphorylation in NCI-H526 cells expressing wild-type Kit (IC50s = 58.1 and 78.9 nM, respectively). It also inhibits VEGF-induced autophosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50 = 64.4 nM). OSI-930 (100 nM) decreases endothelial sprout formation by greater than 50% in isolated rat aortic rings. It reduces tumor growth in a variety of mouse xenograft models, including colon and small-cell lung cancer, melanoma, and glioblastoma models, when administered orally at a dose of 200 mg/kg per day.

Size	5 mg
Shipping	dry ice
CAS Number	728033-96-3
Molecular Formula	C₂₂H₁₆F₃N₃O₂S
SMILES	O=C(C1=C(C=CS1)NCC2=CC=NC3=C2C=CC=C3)NC4=CC=C(OC(F)(F)F)C=C4
Molecular Weight	443,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.49
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.