2016年6月12日星期日

Telatinib|cas 332012-40-5|DC Chemicals

Telatinib|cas 332012-40-5|DC Chemicals

Telatinib(Bay 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.

IC50 value:

Target: multikinase inhibitor

in vitro: Telatinib displays little inhibitory activity against the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, and the Tie-2 receptor .

Product Name: Telatinib|Cat No: DC9586|Cas: 332012-40-5|Molecule Formular: C20H16ClN5O3|Molecule Weight: 409.8257|Other names: Telatinib

Telatinib(Bay 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively.
in vitro: Telatinib displays little inhibitory activity against the Raf kinase pathway, epidermal growth factor receptor family, the fibroblast growth factor receptor (FGFR) family, and the Tie-2 receptor [2]. Telatinib has 0.66, 0.17, and 2.5 times higher IC50 values for VEGFR3, c-Kit, and PDGFRβ than VEGFR2, respectively, while Vatalanib exhibits 18, 20, and 16 times higher IC50 values, respectively, indicating that Telatinib has potential benefit over Vatalanib. Telatinib inhibits VEGFR2 autophosphorylation in a whole-cell assay with an IC50 of 19 nM, suppresses VEGF-dependent proliferation of human umbilical vein endothelial cells with an IC50 of 26 nM, and blocks PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM.
in vivo: Administration of Telatinib as a single agent exhibits a potent anti-tumor activity in multiple human tumor xenograft models including MDA-MB-231 breast cancer, Colo-205 colon cancer, DLD-1 colon cancer, and H460 non-small cell lung cancer, as well as pancreatic and prostate carcinoma in a dose-dependent manner.
For research only, not for human use!

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