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Fexagratinib

CAS No. : 1035270-39-3

MCE 站：Fexagratinib

产品活性：Fexagratinib (AZD4547; ADSK091) 是一种有效的 FGFR 家族抑制剂，作用于 FGFR1，FGFR2，FGFR3 和 FGFR4，IC₅₀ 分别为 0.2 nM，2.5 nM，1.8 nM 和 165 nM。是是

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: Fexagratinib also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC₅₀ of 24 nM. In KG1a, Sum52-PE, MCF7, ａnd KMS11 cell lines, Fexagratinib 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, Fexagratinib potently inhibits FGFR phosphorylation ａnd downstream signaling affected through FRS2, PLCγ, ａnd MAPK at the cellular level.

In Vivo: Female SCID mice bearing KMS11 tumors are randomized ａnd treated chronically with Fexagratinib at a range of well-tolerated doses. Oral Fexagratinib treatment results in dose-dependent tumor growth inhibition. Twice daily administration of Fexagratinib at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily ａnd 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily Fexagratinib results in 65% tumor growth inhibition (P=0.002).

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