Xevinapant hydrochloride

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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:

1071992-57-8

包装与价格：

包装	价格(元)
10mg	电议
50mg	电议

产品介绍

Xevinapant (AT-406) hydrochloride 是一种有效的、口服生物可利用的 Smac 模拟物，也是细胞凋亡蛋白 (IAPs) 抑制剂的拮抗剂。Xevinapant hydrochloride 与 XIAP、cIAP1 和 cIAP2 蛋白结合，Ki 分别为 66.4、1.9 和 5.1 nM。Xevinapant hydrochloride 在无细胞功能测定中有效拮抗 XIAP BIR3 蛋白，诱导细胞 cIAP1 蛋白的快速降解，并抑制各种人类癌细胞系中的癌细胞生长。Xevinapant hydrochloride 在诱导异种移植肿瘤细胞凋亡方面非常有效。

Cas No.	1071992-57-8
别名	AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
分子式	C₃₂H₄₄ClN₅O₄
分子量	598.18
溶解度	DMSO : 175 mg/mL (292.55 mM; Need ultrasonic)
储存条件	Store at -20°C, sealed storage, away from moisture and light
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	Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors[1][2]. Xevinapant (AT-406) hydrochloride potently inhibits cell growth in the MDA-MB-231 breast and SK-OV-3 ovarian cancer cell lines with IC50=144 nM and 142 nM, respectively.Xevinapant (0-3 μM; 0-48 horus) hydrochloride effectively induces cell death in a time- and dose-dependent manner[1]. Xevinapant (AT-406) hydrochloride is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals[1]. Xevinapant hydrochloride evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs[1]. [1]. Cai Q, Sun H, Peng Y, et al. A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment. J Med Chem. 2011;54(8):2714-2726. [2]. Brunckhorst MK, et al. AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer. Cancer Biol Ther. 2012;13(9):804-811.