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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-RGB-286638
RGB-286638

Chemical Structure : RGB-286638

CAS No.: 784210-87-3

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RGB-286638 (RGB286638)

货号: PC-21089Not For Human Use, Lab Use Only.

RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

RGB-286638 is a small-molecule multi-targeted cyclin-dependent kinase (CDK) inhibitor with IC50 of 1-5 nM for cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5.
RGB-286638 is less potent against cyclin H-CDK7 and cyclin D3-CDK6.
RGB-286638 also inhibits several tyrosine and serine/threonine non-CDK enzymes with IC50 of 1-50 nM, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1.
RGB-286638 potently inhibits cell growth of human p53-wt (MM.1S, MM.1R, and H929) and p53-mutant (U266, OPM1, and RPMI) MM cells with EC50 of 20-70 nM.
RGB-286638 (50nM) reduces the phosphorylation of Rb at S807/811 in MM.1S and MM.1R cells, but has no effects on p-Rb S780.
RGB-286638 induces cytotoxicity in p53 knockdown MM.1S, exhibits anti-MM activity in vivo.

物理化学性质&存储条件

分子量 618.56
分子式 C29H37Cl2N7O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N′-4-morpholinylurea hydrochloride (1:2)

参考文献

1. Cirstea D, et al. Leukemia. 2013 Dec;27(12):2366-75.

2. van der Biessen DA, et al. Clin Cancer Res. 2014 Sep 15;20(18):4776-83.

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