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Cdk1/2 Inhibitor III
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cdk1/2 Inhibitor III图片
CAS NO:443798-47-8
包装与价格:
包装价格(元)
10mM 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Cdk1/2 Inhibitor III 是一种有效的 CDK1 和 CDK2 抑制剂,对 CDK1/cyclin B 和 CDK2/cyclin A 的 IC50 分别为 0.6 nM 和 0.5 nM。 Cdk1/2 Inhibitor III 也是一种有效的 CDC2 样激酶 1 (CLK1) 和 CLK3 抑制剂,IC50 分别为 8.9 nM 和 29.2 nM。
Cas No.443798-47-8
化学名5-amino-3-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)-1H-1,2,4-triazole-1-carbothioamide
Canonical SMILESNC1=NC(NC2=CC=C(S(N)(=O)=O)C=C2)=NN1C(NC3=C(F)C=CC=C3F)=S
分子式C15H13F2N7O2S2
分子量425.4
溶解度≤10mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.6 and 0.5 nM forCdk1/cyclin B and Cdk2/cyclin A, respectively

Cdk1/2 Inhibitor III is a Cdk inhibitor.

Cyclin-dependent kinases (CDKs) are a family members of serine-threonine protein kinases responsible for regulation of the eukaryotic cell cycle. Their timed activation guides cells via the cell cycle and ensures the accurate execution of cell division.

In vitro: Cdk1/2 Inhibitor III was identified as a cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A and could less potently inhibit CDC2-like kinases 1 and 3, VEGFR2, and GSK-3β. Cdk1/2 Inhibitor III was found to be lack of effect against a panel of other kinases. Moreover, Cdk1/2 Inhibitor III could block the growth of various cancer cell lines (IC50 values range from 20 to 92 nM) [1].

In vivo: The in-vivo efficacy of compound 3b, a structurally close Cdk1/2 Inhibitor III analog, was examined in the A375 human melanoma cell xenograft model. Doses at 125, 100, and 75 mg/kg were administered once a day for 32 days and tumor size was measured every 4 days. The results showed that in the 125 mg/kg group, there was one nontreatment-related death but the remaining four animals experienced stable disease. In addition, compound 3b administered at 100 and 75 mg/kg led to mean day of survival values of 50.1 and 48.5 days, respectively, with only one treatment-related death in the 100 mg/kg group [1].

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Lin, R. ,Connolly, P.J.,Huang, S., et al. 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: Synthesis and evaluation of biological activities. Journal of Medicinal Chemistry 48(13), 4208-4211 (2005).