Riviciclib (P276-00 free base) 是有效的CDK抑制剂，抑制CDK9-cyclinT1，CDK4-cyclin D1，CDK1-cyclinB的IC50值分别为 20 nM，63 nM，79 nM。Riviciclib 对 Cisplatin 耐药性细胞具有抗肿瘤活性。
| 生物活性 | Riviciclib (P276-00 free base) is a potentcyclin-dependent kinase(CDK)inhibitor, which inhibitsCDK9-cyclinT1,CDK4-cyclin D1, andCDK1-cyclinBwithIC50s of 20 nM, 63 nM, and 79 nM, respectively[1][2].
Riviciclib shows antitumor activity on cisplatin-resistant cells[3]. |
| IC50& Target[1] | CDK9- Cyclin T1 0.020 μM (IC50) | cdk4-cyclin D1 0.063 μM (IC50) | CDK1-Cyclin B 0.079 μM (IC50) | cdk2-cyclin A 0.224 μM (IC50) | cdk2-cyclin E 2.540 μM (IC50) | cdk6-cyclin D3 0.396 μM (IC50) | CDK9-cyclin H 2.900 μM (IC50) |
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体外研究
(In Vitro) | 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[3].
Riviciclib (3-24 hours; 1.5 μM) reduces cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780decrease at 3 h[2].
Riviciclib shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells[2].
Cell Cycle Analysis[3] | Cell Line: | Promyelocytic leukemia cells (HL-60 cells), non-small cell carcinoma (H-460) cells, human normal lung fibroblast (WI-38) cells | | Concentration: | 1.5, 5 μM | | Incubation Time: | 72 hours | | Result: | Showed apoptosis at the end of 24 h and no detectable cells were present in G1 and G2 in HL-60 cells. Caused an exclusive G1 arrest of synchronous population of cancerous cells H-460 cells and normal cells WI-38. |
Western Blot Analysis[2] | Cell Line: | H-460 cells; MCF-7 cells | | Concentration: | 1.5 μM | | Incubation Time: | 3, 6, 9, 12, 24 hours | | Result: | Reduced cyclin D1, Cdk4, and Rb levels in H-460 cells. Rb (retinoblastoma) phosphorylation at Ser780decrease at 3 h. Decreased protein levels of cyclin D1 and Cdk4 levels staring at 6 and 9 h in MCF-7 cells, respectively, and accompanied by a decrease in phosphorylation of Rb at Ser780from 6 h onward, followed by reduced Rb levels at 24 h. |
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体内研究
(In Vivo) | 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[3].
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[3].
| Animal Model: | Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)[3] | | 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)[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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