| 产品描述: | Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL). |
| 靶点: |
CDK9/CycT1:1.68 nM (Ki); CDK9/cyc T2:0.626 nM (Ki); CDK6/cycD1:2.92 nM (Ki); CDK4/Cyc D1:3.96 nM (Ki); CDK1/cycB:5.4 nM (Ki); CDK1/cyc A:9.1 nM (Ki) |
| 体外研究: |
Combination of Voruciclib hydrochloride (200 mpk; Oral gavage) and Venetoclax (10 mpk, 1 mpk, 50 mpk, 25 mpk in U2932, RIVA, SU-DHL-4 and NU-DHL-1, respectively) leads to enhance tumor growth inhibition compared to either drug alone in U2932, RIVA, SU-DHL-4 (six days per week for 4 weeks), and NU-DHL-1 models (five days per week for 3 weeks) of DLBCL[1]. |
| 体内研究: |
Voruciclib hydrochloride (0.5-5 µM; 6 hours) shows targeted downregulation of MCL-1 in both ABC and GCB subtypes. Ki values for each target such as CDK9/cyc T2, CDK9/cyc T1, CDK6/cyc D1, CDK4/cyc D1, CDK1/cyc B, and CDK1/cyc A for Voruciclib hydrochloride are 0.626 nM, 1.68 nM, 2.92 nM, 3.96 nM, 5.4 nM, 9.1 nM, respectively. |
| 参考文献: |
1. Dey J, et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017 Dec 21;7(1):18007. |
| 保存条件: |
-80°C 12个月; -20°C 6个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.975 ml |
9.876 ml |
19.751 ml |
| 5 mM |
0.395 ml |
1.975 ml |
3.95 ml |
| 10 mM |
0.198 ml |
0.988 ml |
1.975 ml |
| 50 mM |
0.04 ml |
0.198 ml |
0.395 ml |
|
| 注意: |
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