AZD4547 | CAS:1035270-39-3

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のAZD4547(CAS:1035270-39-3)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:AZD4547; 
Cat. No. :CS-0971
CAS No. :1035270-39-3
Formula:C26H33N5O3
M. Wt. : 463.57
Solubility:10 mM in DMSO

AZD4547 is a potent inhibitor of the FGFR family with IC50 of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.IC50 & Target: IC50: 0.2 nM (FGFR1), 2.5 nM (FGFR2), 1.8 nM (FGFR3), 165 nM (FGFR4)[1]In Vitro: AZD4547 also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC50 of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, AZD4547 potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC50 values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC50=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC50 values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, AZD4547 potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level[1].In Vivo: Female SCID mice bearing KMS11 tumors are randomized and treated chronically with AZD4547 at a range of well-tolerated doses. Oral AZD4547 treatment results in dose-dependent tumor growth inhibition. Twice daily administration of AZD4547 at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P[1].

Gavine PR, et al. AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family. Cancer Res, 2012, 72(8), 2045-2056.