TAK-960

产品编号 T7200Cas号 1137868-52-0

别名

TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂，IC50为 0.8 nM，对 PLK2 和 PLK3 也有抑制作用，IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖，可治疗多种肿瘤异种移植。

产品编号 T7200Cas号 1137868-52-0

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生物活性

产品描述	TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively.
靶点活性	PLK2:16.9 nM , PLK1:0.8 nM , PLK3:50.2 nM
体外活性	CRC cell lines demonstrated a variable anti-proliferative response to TAK-960 with IC50 values ranging from 0.001 to >?0.75 μmol/L. Anti-proliferative effects were sustained after removal of drug. Following TAK-960 treatment a highly variable accumulation of mitotic (indicating cell cycle arrest) and apoptotic markers was observed. TAK-960 treatment induced G2/M arrest and polyploidy. Six out of the eighteen PDX models responded to single agent TAK-960 therapy (TGII
细胞实验	Fifty-five CRC cell lines and 18 PDX models were exposed to TAK-960 and evaluated for proliferation (IC50) and Tumor Growth Inhibition Index, respectively.?Additionally, 2 KRAS wild type and 2 KRAS mutant PDX models were treated with TAK-960 as single agent or in combination with cetuximab or irinotecan.?TAK-960 mechanism of action was elucidated through immunoblotting and cell cycle analysis[1].

偶联与修饰

抗原信息

存储 & 运输

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 35 mg/mL (62.32 mM)

溶液配制表

DMSO