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.
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].
Cas No.
1137868-52-0
分子式
C27H34F3N7O3
分子量
561.61
储存和溶解度
DMSO:35 mg/mL (62.32 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
m.cnreagent.com