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K03861 Sale

(Synonyms: AUZ454或者K03861,K03861) 目录号 : GC14230

K03861 (K03861) 是一种 II 型 CDK2 抑制剂,Kd 为 8.2 nM。 K03861 (K03861) 通过与活化细胞周期蛋白的结合竞争抑制 CDK2 活性。

K03861 Chemical Structure

Cas No.:853299-07-7

规格 价格 库存 购买数量
5mg
¥998.00
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25mg
¥3,728.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

K03861 is a type II inhibitor of CDK2. The cyclin-dependent kinase holoenzymes contain a catalytic subunit, the Cdk, a family of regulatory subunits, and the cyclins. Cdks are the catalytic subunits of the mammalian heterodimeric serine/threonine kinases progression, Cyclin-dependent kinases (CDKs) play important roles in the cell cycle regulation, transcription, and neuronal function. CDKs are frequently deregulated in some human tumours. The inhibitors targeted CDK are thought to prevent cell proliferation regulating cyclin-CDK complexes. The central role of CDKs in cell cycle regulation makes them a promising target for studying inhibitory molecules that can modify the cell proliferation [1].

K03861 is an aminopyrimidine-phenyl urea inhibitor of CDK2. The type II inhibitor CDK2 cocrystal structure of CDK2 with the inhibitor K03861 revealed a canonical type II binding mode. The type II inhibitors could compete with the binding of cyclins. The residues important for the type II inhibitors may be distant to the ATP binding pockets. The crystal structure of this complex may provide a foundation for the cyclin-competitive CDK2 inhibitors [2].

References:
Malumbres M, Barbacid M.  Mammalian cyclin-dependent kinases[J]. Trends in biochemical sciences, 2005, 30(11): 630-641.
Alexander L T, Mobitz H, Drueckes P, et al.  Type II inhibitors targeting CDK2[J]. ACS chemical biology, 2015, 10(9): 2116-2125.

Chemical Properties

Cas No. 853299-07-7 SDF
别名 AUZ454或者K03861,K03861
化学名 1-(4-((2-aminopyrimidin-4-yl)oxy)phenyl)-3-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)urea
Canonical SMILES CN1CCN(CC2=C(C(F)(F)F)C=C(NC(NC3=CC=C(OC4=NC(N)=NC=C4)C=C3)=O)C=C2)CC1
分子式 C24H26F3N7O2 分子量 501.5
溶解度 ≥ 50.2mg/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。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 1.994 mL 9.9701 mL 19.9402 mL
5 mM 0.3988 mL 1.994 mL 3.988 mL
10 mM 0.1994 mL 0.997 mL 1.994 mL
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