产品
编 号：F281885
分子式：C31H31N5O6S3
分子量：665.8
分子式：C31H31N5O6S3
分子量：665.8
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 2250404-95-4
产品详情
生物活性：
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
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.
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.
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
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.
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.
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