Cdk1/2 Inhibitor III

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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。

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 SMILES	NC1=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 tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation 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).