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Cdk1/2 Inhibitor III Sale

(Synonyms: Cyclin-dependent kinase 1/2 Inhibitor III) 目录号 : GC14294

A cell-permeable inhibitor of Cdk1 and Cdk2

Cdk1/2 Inhibitor III Chemical Structure

Cas No.:443798-47-8

规格 价格 库存 购买数量
10mM 1 mL in DMSO
¥3,140.00
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5mg
¥2,855.00
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10mg
¥4,589.00
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50mg
¥13,256.00
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100mg
¥20,394.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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).

Chemical Properties

Cas No. 443798-47-8 SDF
别名 Cyclin-dependent kinase 1/2 Inhibitor III
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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.3507 mL 11.7536 mL 23.5073 mL
5 mM 0.4701 mL 2.3507 mL 4.7015 mL
10 mM 0.2351 mL 1.1754 mL 2.3507 mL
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