Telatinib

Telatinib       
 
        上海义森生物科技有限公司

 

                                                                                                                                                                             

技术数据:

分子量(MW):	409.83
化学式:	C20H16ClN5O3
溶解度:	DMSO 82mg/mL   Water <1mg/mL   Ethanol 1mg/mL
纯度:	>97%
稳定性:	at -20℃ 2 years
CAS号:	332012-40-5, 332013-24-8 (4-methylbenzenesulfonate), 332013-28-2 (2HCl)

生物活性

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. ^[1][2][3]