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Riviciclib hydrochloride

CAS No. : 920113-03-7

MCE 站：Riviciclib hydrochloride

产品活性：Riviciclib hydrochloride (P276-00) 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 hydrochloride (P276-00) 对 Cisplatin 耐药性细胞具有抗肿瘤活性。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: Riviciclib hydrochloride (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 hydrochloride (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 hydrochloride shows activity in human cancer cell lines, such as colon carcinoma, osteosarcomal, cervical carcinoma, and bladder carcinoma cells.

In Vivo: Riviciclib hydrochloride (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 hydrochloride (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 inhibited growth.

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