Riviciclib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型有效的 CDK 抑制剂，对 Cdk4/cyclin D1、Cdk1/cyclin B 和 Cdk9/cyclin T1 的 IC50 分别为 79 nM、63 nM 和 20 nM。

A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively; weakly inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk6/cyclin D3 and Cdk7/cyclin H with IC50 of 0.2-3 uM; shows potent antiproliferative effects against various human cancer cell lines (IC50=200-800 nM); induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.Pancreatic Cancer Phase 2 Clinical.

Cell Cycle Analysis Cell Line:Promyelocytic leukemia cells (HL-60 cells), non-small cell carcinoma (H-460) cells, human normal lung fibroblast (WI-38) cellsConcentration: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 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 Ser780 decrease 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 Ser780 from 6 h onward, followed by reduced Rb levels at 24 h.

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.

P276-00 hydrochloride

Cell Cycle/DNA Damage

CDK

CDK1/CyclinB| CDK2/CyclinA| CDK4/CyclinD1| CDK6/CyclinD3| CDK9/CyclinT1

Cancer

Pancreatic Cancer

920113-03-7

438.3

C21H20ClNO5.HCl

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (114.08 mM)

CN1CCC(C1CO)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl

2-(2-chlorophenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one hydrochloride

(-20℃)

With Ice Pack

≥ 2 years