货号	规格	价格	上海	北京	珠海	重庆	武汉
S87648-5mg促销	98.60%	￥245.00 ￥196.00 S87648-5mg ￥196.00 现货	5 5	-	-	-	-
S87648-10mg促销	98.60%	￥450.00 ￥360.00 S87648-10mg ￥360.00 现货	3 3	-	-	-	-
S87648-25mg促销	98.60%	￥850.00 ￥680.00 S87648-25mg ￥680.00 现货	4 4	-	-	-	-
S87648-100mg促销	≥98%	￥2150.00 ￥1930.00 S87648-100mg ￥1930.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG

靶点：

Hec1/Nek2;Apoptosis; MicrotubuleAssociated

体外研究：

T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM). T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells. T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner. T-1101 tosylate (1 µM; 24 hours) induces apoptosis. T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1. Apoptosis Analysis Cell Line: HeLa cells Concentration: 1 µM Incubation Time: 24 hours Result: Increased the amount of apoptotic marker proteins cleaved caspase-3 and PARP and decreased the amount of antiapoptotic proteins Mcl-1 and XIAP in HeLa cells. Western Blot Analysis Cell Line: K562 cells Concentration: 1 μM Incubation Time: 3 hours, 6 hours, 16 hours, 24 hours Result: Lowered the level of Nek2 in a time-dependent manner.

体内研究：

T-1101 tosylate shows good oral bioavailability and thermal stability. Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) halves the dose of sorafenib (25 mg/kg to 12.5 mg/kg) required to exhibit comparable in vivo activity towards Huh-7 xenografts. T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts. Animal Model: SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts Dosage: 25 mg/kg, 50 mg/kg Administration: Oral administration; twice per day; 28 days Result: Showed significant in vivo activity in mice bearing various human cancer xenografts.

参考文献：

1. Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.502 ml	7.51 ml	15.02 ml
5 mM	0.3 ml	1.502 ml	3.004 ml
10 mM	0.15 ml	0.751 ml	1.502 ml
50 mM	0.03 ml	0.15 ml	0.3 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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