TAK-960
作者：齐岳
发布时间：2023-09-13
09:13:11
点击数：
产品名称：TAK-960
产品描述：
| 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<?20). The addition of TAK-960 to standard of care chemotherapy resulted in largely additive antitumor effects[1]. |
| 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]. |
| 分子量 | 561.6 |
| 分子式 | C27H34F3N7O3 |
| CAS No. | 1137868-52-0 |
存储
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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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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