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  • 827318-97-8

827318-97-8

PHA-739358
827318-97-8
询价 5kg 起订
10kg 起订
25kg 起订
广东 更新日期:2024-12-06

广州优南科技有限公司

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产品详情:

英文名称:
PHA-739358
CAS号:
827318-97-8
纯度规格:
>98% HPLC
产品类别:
医药级

Danusertib 是一种极光激酶 (aurora kinase) 抑制剂,能够抑制 Aurora A,Aurora B 和 Aurora C 的活性,IC50 值分别为 13,79 和 61 nM。

Danusertib (0.01 to 50 μM) significantly decreases viability of C13 and A2780cp cells. The IC50s are 10.40 and 1.83 μM for C13 cells, and 19.89 and 3.88 μM for A2780cp cells after 24- and 48-h treatment. Danusertib induces cell cycle arrest in G2/M phase in C13 and A2780cp cells. Danusertib treatment results in a marked increase in the percentage of cells arrested in G2/M phase and an accumulation of polyploidy in C13 and A2780cp cells. Danusertib demotes the expression of CDK1/CDC2 and cyclin B1 but promotes the expression of p21 Waf1/Cip1, p27 Kip1, and p53. Danusertib induces autophagy in C13 and A2780cp cells with the involvement of PI3K/Akt/mTOR signaling pathway[1]. PHA-739358 strongly inhibits proliferation of all leukemic cell lines tested, with IC50 values ranging from 0.05 μM to 3.06 μM. PHA-739358 induces antiproliferative effects in BaF3-p210 cells, including IM-resistant M351T, E255K, and T315I mutants. PHA-739358 (5 μM) reduces phosphorylation of CrkL in BaF3-p210 wt cells and IM-resistant mutants[2]. Danusertibsertib leads to cell-cycle arrest and completely inhibits cell proliferation of the GEP-NET cells in vitro[3].

PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period[2]. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil[3].

827318-97-8;

公司简介

广州优南科技有限公司,是一家集研发、生产、销售于一体的高新技术企业,为全球生物医药企业、高校及科研院提供生命科学研究的产品与服务。 优南拥有自主研发的品牌ULS,为客户提供超过50000的工具化合物(小分子抑制剂/激动剂、标准品/对照品、荧光标记染料及探针)、医药原料及中间体、新型材料。

成立日期 (7年)
注册资本 100万
员工人数 10-50人
年营业额 ¥ 100万以内
经营模式 贸易,工厂,试剂,定制,服务
主营行业 有机光电,医药中间体,生物活性小分子,原料药

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