CPL304110,1627826-19-0

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CPL304110

CAS No. : 1627826-19-0

MCE 国际站：CPL304110

产品活性：CPL304110 是有效的、口服有效的、选择性的成纤维细胞生长因子受体 FGFR (1-3) 的抑制剂，其对 FGFR (1-3) 的 IC₅₀ 值分别为 0.75 nM、0.5 nM 和 3.05 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：FGFR

In Vitro: CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK).
CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC₅₀ of 85.64 nM.
CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases.

In Vivo: CPL304110 (p.o., 40 mg/kg) exhibits a t_1/2 of 2 h and C_max of 3369 ng/mL in mice.
CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day.

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