产品
编 号：F748695
分子式：C21H27FN8S
分子量：442.56
分子式：C21H27FN8S
分子量：442.56
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
结构图
CAS No: 2078047-99-9
产品详情
生物活性：
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.
体内研究：
CDK4/6-IN-15 (compound 91) (2 mg/kg for i.v. or 10 mg/kg for p.o.; single dose) shows comparable oral absorption in healthy male adult BALB/c mice (20-25 g) as well as (5 mg/kg for i.v. or 200 mg/kg for p.o.; single dose) in male albino Wistar rats (250-350 g).Pharmacokinetic AnalysisRouteDose (mg/kg)CL (mL/min/kg)Vss (L/kg)AUC (μM·h)Cmax (μM)Tmax (h)t1/2 (h)F (%)
ratIV515527.51.21.4/2.1/
PO20//4.40.34.320.395
mouseIV29015.70.71.3/2.9/
PO10//4.30.62.52.7129
体外研究：
CDK4/6-IN-15 (compound 91) (10 μM; 24 h) also potently inhibits FLT3 and MYLK4 with inhibition rates >90%.CDK4/6-IN-15 (0-5 μM; 72 h) suppresses tumour cell proliferation selectively with GI50s of 0.107 μM (MV4-11) and 0.325 μM (MDA-MB-453).CDK4/6-IN-15 (0.1-1 μM; 24 h) arrests exclusively the cell cycle at G1 phase in Rb-positive MV4-11 cells and MDA-MB-453 cells.CDK4/6-IN-15 (0.1-1 μM or 0.3-3 μM; 24-96 h) triggers apoptosis in MV4-11 and MDA-MB-453 cells.CDK4/6-IN-15 (0.1-3.3 μM; 4-24 h) inhibits phosphorylation of Rb.
CDK4/6-IN-15 is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 potently inhibits cancer cells growth. CDK4/6-IN-15 arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.
体内研究：
CDK4/6-IN-15 (compound 91) (2 mg/kg for i.v. or 10 mg/kg for p.o.; single dose) shows comparable oral absorption in healthy male adult BALB/c mice (20-25 g) as well as (5 mg/kg for i.v. or 200 mg/kg for p.o.; single dose) in male albino Wistar rats (250-350 g).Pharmacokinetic AnalysisRouteDose (mg/kg)CL (mL/min/kg)Vss (L/kg)AUC (μM·h)Cmax (μM)Tmax (h)t1/2 (h)F (%)
ratIV515527.51.21.4/2.1/
PO20//4.40.34.320.395
mouseIV29015.70.71.3/2.9/
PO10//4.30.62.52.7129
体外研究：
CDK4/6-IN-15 (compound 91) (10 μM; 24 h) also potently inhibits FLT3 and MYLK4 with inhibition rates >90%.CDK4/6-IN-15 (0-5 μM; 72 h) suppresses tumour cell proliferation selectively with GI50s of 0.107 μM (MV4-11) and 0.325 μM (MDA-MB-453).CDK4/6-IN-15 (0.1-1 μM; 24 h) arrests exclusively the cell cycle at G1 phase in Rb-positive MV4-11 cells and MDA-MB-453 cells.CDK4/6-IN-15 (0.1-1 μM or 0.3-3 μM; 24-96 h) triggers apoptosis in MV4-11 and MDA-MB-453 cells.CDK4/6-IN-15 (0.1-3.3 μM; 4-24 h) inhibits phosphorylation of Rb.
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