IACS-10759 Hydrochloride

立即咨询

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1807523-99-4

IACS-10759 Hydrochloride 是一种具有口服活性的强效线粒体复合物 I 的氧化磷酸化 (OXPHOS) 抑制剂。 IACS-10759 Hydrochloride 在依赖 OXPHOS 的脑癌和急性髓性白血病 (AML) 模型中抑制增殖并诱导细胞凋亡。 IACS-10759 Hydrochloride 具有用于复发/难治性 AML 和实体瘤研究的潜力。

Cas No.	1807523-99-4
别名	IACS-10759 hydrochloride
Canonical SMILES	FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCC(S(=O)(C)=O)CC5)=CC=C4)C(C)=N3)=N2)C=C1.Cl
分子式	C₂₅H₂₆ClF₃N₆O₄S
分子量	599.02
溶解度	DMSO: ≥ 100 mg/mL (166.94 mM); Water:< 0.1 mg/mL (insoluble)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	IACS-10759 Hydrochloride is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS). OXPHOS[1] IACS-10759 inhibits the conversion of NADH to NAD+ in an immunoprecipitated complex I assay at low nM concentrations[1]. 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[1]. [1]. Protopopova M. IACS-10759: A novel OXPHOS inhibitor which selectively kill tumors with metabolic vulnerabilities. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 4380. doi:10.1158/1538-7445.AM2015-4380