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抑制剂描述:

产品名称:IACS-010759

产品别名:见爱必信官网

英文别名:IACS-010759

靶点:OxPhos

CAS:1570496-34-2

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

IACS-010759  is a potent and selective oxidative phosphorylation inhibitor (IC50 < 10 nM) that blocks cellular respiration through inhibition of complex I.

溶解性:DMSO :27 mg/mL (47.99 mM)

体外研究:

IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations.

体内研究:IACS-10759 is orally bioavailable with excellent physicochemical properties in preclinical species and achieves significant in vivo efficacy with daily oral dosing of 10-25 mg/kg. There is a >50 day extension of median survival in an orthotopic AML cell line xenograft and robust regression in DLBCL and GBM xenograft models.

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