Territorial Availability: Available through Bertin Technologies only in France
- Synonyms
- N-methyl-4-[4-[[3-(trifluoromethyl)benzoyl]amino]phenoxy]-2-pyridinecarboxamide
- Correlated keywords
- VEGFR FGFR 2 anti-tumor SKLB 610 PI-3-K Cdk-2 6 D-3 A-549 HCT-116 MDAMB231 MDAMB-231 MDA-MB231 DU-145
- Product Overview:
SKLB610 is an inhibitor of VEGF receptor 2 (VEGFR2).{52033} It inhibits VEGFR2 activity by 97% but also inhibits FGFR2 and PDGFR? activity by 65 and 55%, respectively, when used at a concentration of 10 µM. It is selective for VEGFR2, FGFR2, and PDGFR? over PI3K, EGFR, Aurora A, Cdk2/cyclin E, and Cdk6/cyclin D3 at 10 µM. SKLB610 inhibits phosphorylation of VEGFR2 induced by VEGF in human umbilical vein endothelial cells (HUVECs). It inhibits proliferation of HUVECs induced by VEGF and basic FGF (bFGF; IC50s = 2.2 and 4.7 µM, respectively). It also inhibits HUVEC capillary tube formation and migration when used at concentrations of 2.5 and 10 µM, respectively. SKLB610 inhibits proliferation of a variety of cancer cells, including A549 human lung cancer, HCT116 human colorectal carcinoma, MDA-MB-231 human mammary carcinoma, Raji human Burkitt’s lymphoma, and DU145 human prostate cancer cells (IC50s = 5.7, 5.3, 25.6, 6.4, and 6.3 µM, respectively). It reduces tumor growth in A549 and HCT116 mouse xenograft models when administered at a dose of 50 mg/kg per day.
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.