Vatalanib (PTK787) 2HCl

Short Summary : Tyrosine kinase receptor inhibitor

Category : Tyrosine Kinase|VEGFR

Purity : 0.98

CAS Number : 212141-51-0

Formula : C20H15ClN4.2HCl

Molecular Weight : 419.73

SMILE : C1=CC=C2C(=C1)C(=NN=C2NC3=CC=C(C=C3)Cl)CC4=CC=NC=C4.Cl.Cl

Solubility : >21mg/mL in DMSO

Storage : Store at -20°C

Description : 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 M, 0.077 M and 0.27 M 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 tyrosine kinase (PDGFR-), c-Kit and c-Fms, to a lesser degree with IC50 values of 0.58 M, 0.73 M and 1.4 M respectively [1]. Vatalanib has been found to be potentially therapeutic for the treatment of angiogenesis-related diseases including solid tumors [1].References:[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.

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