CPL304110 |
| カタログ番号GC62274 |
CPL304110 は、線維芽細胞増殖因子受容体 FGFR (1-3) の強力な経口活性および選択的阻害剤であり、FGFR の IC50 値はそれぞれ 0.75 nM、0.5 nM、および 3.05 nM (1-3) です。
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Cas No.: 1627826-19-0
Sample solution is provided at 25 µL, 10mM.
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CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3), with IC50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively[1].
CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK)[1].CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC50 of 85.64 nM[1].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[1].
CPL304110 (p.o., 40 mg/kg) exhibits a t1/2 of 2 h and Cmax of 3369 ng/mL in mice[1].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[1].
[1]. Abdellah Yamani, et al. Discovery and optimization of novel pyrazole-benzimidazole CPL304110, as a potent and selective inhibitor of fibroblast growth factor receptors FGFR (1-3). Eur J Med Chem. 2020 Nov 7;112990.
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