TAK-960
作者：齊岳
發(fā)布時間：2023-09-13
09:13:11
點(diǎn)擊數(shù)：
產(chǎn)品名稱：TAK-960
產(chǎn)品描述：
| 產(chǎn)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. |
| 靶點(diǎn)活性 | PLK2:16.9 nM , PLK1:0.8 nM , PLK3:50.2 nM |
| 體外活性 | 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<?20). The addition of TAK-960 to standard of care chemotherapy resulted in largely additive antitumor effects[1]. |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 分子量 | 561.6 |
| 分子式 | C27H34F3N7O3 |
| CAS No. | 1137868-52-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 35 mg/mL (62.32 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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