Tyrosine kinase receptor inhibitor
CAS：212141-51-0
分子式：C20H15ClN4.2HCl
分子量：419.73
纯度：98%
存储：Store at -20°C

Background:

Vatalanib, also known as PTK787, is a potent vascular endothelial growth factor (VEGF) receptor tyrosine kinases inhibitor that inhibits VEGF receptor/KDR, VEGF receptor/Flt-1 and VEGF receptor/Flk with the half maximal inhibition concentration IC50 values of 0.037 μM, 0.077 μM and 0.27 μM respectively [1].

Vatalanib also inhibits other tyrosine kinases belonging to the same family of tyrosine kinase receptors as the VEGF receptors, including the platelet-derived growth factor receptor β tyrosine kinase (PDGFR-β), c-Kit and c-Fms, to a lesser degree with IC50 values of 0.58 μM, 0.73 μM and 1.4 μM respectively [1].

Vatalanib has been found to be potentially therapeutic for the treatment of angiogenesis-related diseases including solid tumors [1].

参考文献:
[1] Wood JM, Bold G, Buchdunger E, Cozens R, Ferrari S, Frei J, Hofmann F, Mestan J, Mett H, O'Reilly T, Persohn E, R?sel J, Schnell C, Stover D, Theuer A, Towbin H, Wenger F, Woods-Cook K, Menrad A, Siemeister G, Schirner M, Thierauch KH, Schneider MR, Drevs J, Martiny-Baron G, Totzke F. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000 Apr 15;60(8):2178-89.