产品
编 号：F754712
分子式：C24H27ClFN7O
分子量：483.97
分子式：C24H27ClFN7O
分子量：483.97
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CAS No: 2699091-15-9
产品详情
生物活性：
CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.
体内研究：
CDK4/6-IN-14 (compound 42; 100-150 mg/kg; p.o; once a day; for 23 days) significantly inhibits tumor growth of the MCF-7 xenograft model. CDK4/6-IN-14 (compound 42) exhibits a suitable t1/2 of intravenous and oral administration (2.62 and 3.59 h, respectively). Moreover, the oral bioavailability of CDK4/6-IN-14 is 43%. Pharmacokinetic Parameters of CDK4/6-IN-14 (Compound 42) in Sprague–Dawley Rats.admin.Cmax (ng/mL) AUC0-∞ (h × ng/mL) MRT0-∞ (h) Tmax (h) t1/2 (h) F (%)
IV290.52372.563.500.0332.62
PO144.111612.189.1163.5943
Dose: i.v. at 1 mg/kg; p.o. at 10 mg/kgAnimal Model:BALB/c nude mice bearing MCF-7 cells
Dosage:100 mg/kg, 150 mg/kg
Administration:Orally administertion; once a day; for 23 days
Result:Significantly inhibited tumor growth of the MCF-7 xenograft model.
体外研究：
CDK4/6-IN-14 (compound 42; 1-6 μM; 5 days) exhibits potent inhibitory activity against the proliferation of breast cancer MCF-7, T47D, and ZR-75-1 cell lines. CDK4/6-IN-14 significantly inhibits growth and clone formation of MCF-7 and T47D cells.CDK4/6-IN-14 (compound 42; 1-6 μM) arrests the cell cycle at the G1 phase of MCF-7 and T47D cells in the dose-dependent manner.CDK4/6-IN-14 (compound 42; 1-6 μM; 24 hours) significantly inhibits the phosphorylation of retinoblastoma (RB), while the expression of RB protein was almost unchanged. In addition, CDK4/6-IN-14 exhibits a concentration-dependent effect to decrease the level of c-MYC and cyclin D1.
CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC50s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.
体内研究：
CDK4/6-IN-14 (compound 42; 100-150 mg/kg; p.o; once a day; for 23 days) significantly inhibits tumor growth of the MCF-7 xenograft model. CDK4/6-IN-14 (compound 42) exhibits a suitable t1/2 of intravenous and oral administration (2.62 and 3.59 h, respectively). Moreover, the oral bioavailability of CDK4/6-IN-14 is 43%. Pharmacokinetic Parameters of CDK4/6-IN-14 (Compound 42) in Sprague–Dawley Rats.admin.Cmax (ng/mL) AUC0-∞ (h × ng/mL) MRT0-∞ (h) Tmax (h) t1/2 (h) F (%)
IV290.52372.563.500.0332.62
PO144.111612.189.1163.5943
Dose: i.v. at 1 mg/kg; p.o. at 10 mg/kgAnimal Model:BALB/c nude mice bearing MCF-7 cells
Dosage:100 mg/kg, 150 mg/kg
Administration:Orally administertion; once a day; for 23 days
Result:Significantly inhibited tumor growth of the MCF-7 xenograft model.
体外研究：
CDK4/6-IN-14 (compound 42; 1-6 μM; 5 days) exhibits potent inhibitory activity against the proliferation of breast cancer MCF-7, T47D, and ZR-75-1 cell lines. CDK4/6-IN-14 significantly inhibits growth and clone formation of MCF-7 and T47D cells.CDK4/6-IN-14 (compound 42; 1-6 μM) arrests the cell cycle at the G1 phase of MCF-7 and T47D cells in the dose-dependent manner.CDK4/6-IN-14 (compound 42; 1-6 μM; 24 hours) significantly inhibits the phosphorylation of retinoblastoma (RB), while the expression of RB protein was almost unchanged. In addition, CDK4/6-IN-14 exhibits a concentration-dependent effect to decrease the level of c-MYC and cyclin D1.
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