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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-MELK-HTH-01-091
HTH-01-091

Chemical Structure : HTH-01-091

CAS No.: 2000209-42-5

HTH-01-091 (MELK inhibitor)

货号: PC-61763Not For Human Use, Lab Use Only.

HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.

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5 mg ¥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.
HTH-01-091 displays no significant activity for PIK3CA, mTOR, GSK3A and CDK7 (IC50>600 nM); exhibits substantially improved kinome selectivity in comparison with OTSSP167.
HTH-01-091 induces MELK degradation, but demonstrates poor antiproliferative effects in basal-like breast cancer cell lines.

物理化学性质&存储条件

分子量 499.436
分子式 C26H28Cl2N4O2
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

9-(3,5-dichloro-4-hydroxyphenyl)-1-((1r,4r)-4-((dimethylamino)methyl)cyclohexyl)-3,4-dihydropyrimido[5,4-c]quinolin-2(1H)-one

参考文献

1. Huang HT, et al. Elife. 2017 Sep 19;6. pii: e26693.

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