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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Aurora Kinase-Danusertib
Danusertib

Chemical Structure : Danusertib

CAS No.: 827318-97-8

Danusertib (PHA-739358; PHA739358; PHA 739358)

货号: PC-42422Not For Human Use, Lab Use Only.

Danusertib (PHA-739358) is a potent, ATP-competitive Aurora kinase inhibitor with IC50 of 13,79 and 61 nM for Aurora A, B and C, respectively.

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10 mg ¥1280 In stock
25 mg ¥1980 In stock
50 mg ¥2980 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

Danusertib (PHA-739358) is a potent, ATP-competitive Aurora kinase inhibitor with IC50 of 13,79 and 61 nM for Aurora A, B and C, respectively.
Danusertib (PHA-739358) also inhibits Abl, RET, and FGFR1 (IC50=25,31, and 47 nM), efficiently inhibits imatinib-resistant Abl mutant T315I (IC50=5 nM)。
Danusertib (PHA-739358) inhibits phosphorylation of histone H3 in Ser10, and has significant antitumor activity in different xenografts and spontaneous and transgenic animal tumor models.

物理化学性质&存储条件

分子量 474.5548
分子式 C26H30N6O3
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

DMSO: 7.5 mg/mL

Chemical Name/SMILES

Benzamide, 4-(4-methyl-1-piperazinyl)-N-[1,4,5,6-tetrahydro-5-[(2R)-2-methoxy-2-phenylacetyl]pyrrolo[3,4-c]pyrazol-3-yl]-

参考文献

1. Fancelli D, et al. J Med Chem. 2006 Nov 30;49(24):7247-51.

2. Modugno M, et al. Cancer Res. 2007 Sep 1;67(17):7987-90.

3. Carpinelli P, et al. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68.

4. Gontarewicz A, et al. Blood. 2008 Apr 15;111(8):4355-64.

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