产品
编 号：F068894
分子式：C26H24ClN3O3
分子量：461.94
分子式：C26H24ClN3O3
分子量：461.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1202916-90-2
产品详情
生物活性：
CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
体内研究：
CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models.Animal Model:Nude mice, MV-4-11 xenograft models
Dosage:50 mg/kg, 100 mg/kg
Administration:Oral administration; once daily; over a period of 21 days
Result:Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
体外研究：
CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.CX-6258 treatment results in a significant reduction in NKX3.1 half-life.
CX-6258 is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
体内研究：
CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models.Animal Model:Nude mice, MV-4-11 xenograft models
Dosage:50 mg/kg, 100 mg/kg
Administration:Oral administration; once daily; over a period of 21 days
Result:Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
体外研究：
CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.CX-6258 treatment results in a significant reduction in NKX3.1 half-life.
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