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编 号：F520785
分子式：C21H20ClNO5
分子量：401.84
分子式：C21H20ClNO5
分子量：401.84
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CAS No: 920113-02-6
产品详情
生物活性：
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively.Riviciclib shows antitumor activity on cisplatin-resistant cells.
体内研究：
Riviciclib (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft.Riviciclib (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibits growth.Animal Model:Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)
Dosage:35 mg/kg
Administration:Administered i.p.; daily for 10 days
Result:Given 35 mg/kg showed significant inhibition in the growth.
Animal Model:Human xenograft model with H-460 tumor xenograft (severe combined immunodeficient mice)
Dosage:50 mg/kg; 30 mg/kg
Administration:Administered i.p.; 50 mg/kg once daily for 20 days; Administered i.p.; 30 mg/kg twice daily for 18 treatments
Result:Given 50 mg/kg and 30 mg/kg twice daily significantly inhibited growth.
体外研究：
Riviciclib (1.5-5 μM; 72 hours) shows no detectable cells in G1 and G2 in promyelocytic leukemia cells and arrest of cells in G1 in synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells.Riviciclib (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h. Riviciclib shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells.
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively.Riviciclib shows antitumor activity on cisplatin-resistant cells.
体内研究：
Riviciclib (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft.Riviciclib (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibits growth.Animal Model:Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)
Dosage:35 mg/kg
Administration:Administered i.p.; daily for 10 days
Result:Given 35 mg/kg showed significant inhibition in the growth.
Animal Model:Human xenograft model with H-460 tumor xenograft (severe combined immunodeficient mice)
Dosage:50 mg/kg; 30 mg/kg
Administration:Administered i.p.; 50 mg/kg once daily for 20 days; Administered i.p.; 30 mg/kg twice daily for 18 treatments
Result:Given 50 mg/kg and 30 mg/kg twice daily significantly inhibited growth.
体外研究：
Riviciclib (1.5-5 μM; 72 hours) shows no detectable cells in G1 and G2 in promyelocytic leukemia cells and arrest of cells in G1 in synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells.Riviciclib (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780 decrease at 3 h. Riviciclib shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells.
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