WZ4002

WZ4002

WZ4002

Cat.No.ABP000892 Chemical NameWZ4002 CAS1213269-23-8 MolFormulaC25H27ClN6O3 MolWeight494.973 Purity >99%

Chemical Name : WZ4002

CAS : 1213269-23-8

Synonyms: N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide

Storage:at -20℃ 2 years

Biologieal

Telatinib (BAY 57-9352) is an orally available, potent multitargeted VEGFR-2, VEGFR-3, PDGFR-β and c-Kit tyrosine kinases inhibitor with an IC50 of 19 nM for the inhibition of VEGFR-2 autophosphorylation. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) also inhibits VEGF-dependent proliferation of human umbilical vein endothelial cells (HUVECs) with an IC50 of 26 nM and PDGF-stimulated growth of human aortic smooth muscle cells with an IC50 of 249 nM. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) demonstrates anti-tumor activity in various cancer models. Formation of the N-glucuronides of telatinib is identified as the major biotransformation pathway in man. Telatinib (BAY 57-9352, CP 127374; KOS 953; NSC 330507; Tanespimycin) is metabolized by various CYP isoforms and UGT1A4

Reference

[1] Steeghs N et al. Clin Cancer Res. 2008 Jun 1; 14(11):3470-6.

[2] Eskens FA et al. J Clin Oncol. 2009 Sep 1; 27(25):4169-76.

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