TAK-960|cas:1137868-52-0|西域试剂

TAK-960,99.75%

产品编号：Bellancom-15160| CAS NO：1137868-52-0| 分子式：C₂₇H₃₄F₃N₇O₃| 分子量：561.60

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15160	￥866.00	杭州北京（现货）
Bellancom-15160	￥1300.00	杭州北京（现货）
Bellancom-15160	￥1800.00	杭州北京（现货）
Bellancom-15160	￥5400.00	杭州北京（现货）
Bellancom-15160	￥8400.00	杭州北京（现货）

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TAK-960

产品介绍

TAK-960 是一种有效的，可口服的，选择性的 polo-like kinase 1 (PLK1) 抑制剂，IC₅₀ 为 0.8 nM。TAK-960 对 PLK2 和 PLK3 也有抑制作用，IC₅₀ 分别为 16.9 和 50.2 nM。TAK-960 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。

生物活性

TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts.

体外研究

TAK-960 treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC₅₀ values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells.
TAK-960 (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells
Concentration:	2-1000 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.

体内研究
(In Vivo)

TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts.
In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)
Dosage:	10 mg/kg
Administration:	P.o.; once daily for 2 weeks
Result:	Substantial antitumor activity and good tolerability.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)
Dosage:	10 mg/kg
Administration:	P.o.; once daily for 2 weeks
Result:	Substantial antitumor activity and good tolerability.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)
Dosage:	10 mg/kg
Administration:	P.o.; once daily for 2 weeks
Result:	Substantial antitumor activity and good tolerability.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (29.68 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7806 mL	8.9031 mL	17.8063 mL
5 mM	0.3561 mL	1.7806 mL	3.5613 mL
10 mM	0.1781 mL	0.8903 mL	1.7806 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式