Venetoclax - CAS:1257044-40-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Venetoclax 促销
英文名称:	Venetoclax
别名:	4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
CAS No:	1257044-40-8	分子式:	C₄₅H₅₀ClN₇O₇S	分子量:	868.44
CAS No:	1257044-40-8
分子式:	C₄₅H₅₀ClN₇O₇S
分子量:	868.44

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V10012 Venetoclax ≥98%（HPLC） (psaitong)

相关产品

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(100mg/mL)

产品描述：

基本信息

产品编号：V10012
产品名称：Venetoclax (ABT199)
CAS:	1257044-40-8	储存条件	粉末	-20℃	四年

分子式：	C45H50ClN7O7S		溶于液体	-80℃	六个月
分子量	868.44			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	100mg/mL (115.14mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）	5% DMSO+50% PEG 300+5% Tween 80+ddH2O	5mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.1515mL	5.7575mL	11.5149mL
5mM	0.2303mL	1.1515mL	2.3030mL
10mM	0.1151mL	0.5757mL	1.1515mL
50mM	0.0230mL	0.1151mL	0.2303mL

生物活性

产品描述	一种口服的、选择性的Bcl-2抑制剂，具有潜在的抗肿瘤活性，Ki＜0.01nM。
靶点/IC50	Bcl-2 0.01nM (Ki)	Bcl-xL 48nM (Ki)	Bcl-W 245nM (Ki)
体外研究	Venetoclax (ABT-199) potently kills FL5.12-BCL-2 cells (EC50=4nM),Venetoclax (ABT-199) shows much weaker activity against FL5.12-BCL-XL cells (EC50=261nM). ABT-199 also shows selectivity in cellular mammalian two-hybrid assays, where it disrupts BCL-2-BIM complexes (EC50=3nM) but is much less effective against BCL-XL-BCL-XS (EC50=2.2μM) or MCL-1-NOXA complexes.
体内研究	After a single oral dose of 12.5mg per kg body weight in xenografts derived from RS4;11 cells (ALL), Venetoclax (ABT-199) causes a maximal tumor growth inhibition (TGImax) of 47% (P<0.001) and tumor growth delay (TGD) of 26% (P<0.05).Treatment of established xenografted (a mouse xenograft model of the T-ALL cell line LOUCY) tumors with Venetoclax (ABT199) 100mg/kg for 4 days results in a significant reduction of leukemic burden.

推荐实验方法(仅供参考)

激酶实验：

亲和力分析

竞争性荧光偏振检测测定ABT-199对Bcl-2家族的不同亚型的亲和力(Ki 或 IC50)。使用如下肽探针/蛋白对：f-bad (1nM) 与Bcl-xL (6nM), f-Bax (1nM) 与 Bcl-2 (10nM),f-Bax(1nM) 与Bcl-w (40nM), f-Noxa(2nM) 与Mcl-1 (40nM), 及 f-Bax (1 nM)与Bcl-2-A1(15 nM)。使用时间分辨荧光共振能量转移检测测定对Bcl-xL的亲和力。Bcl-xL (1nM, His标记的 ) 与200nM f-Bak, 1nM Tb标记的anti-His抗体, 及 ABT-199，在室温下混合30分钟。在Envision酶标仪上，使用340/35nm 激发滤光片及520/525 (f-Bak) 和495/510nm (Tb标记的anti-His抗体) 发射滤光片，测量荧光值。

细胞实验:

RS4;11 cells are seeded at 50,000 per well in 96-well plates and treated with compounds diluted in half-log steps starting at 1μM and ending at 0.00005μM. All other leukemia and lymphoma cell lines are seeded at 15,000-20,000 cells per well in the appropriate medium and incubated with Venetoclax or Navitoclax for 48 h. Effects on proliferation are determined using Cell TiterGlo reagent. EC50 values are determined by nonlinear regression analysis of the concentration response data.Mouse FL5.12-BCL-2 and FL5.12-BCL-XL cells are propagated and assessed. Bak-/- Bax-/- double knockout mouse embryonic fibroblasts are seeded into 96-well microtiter plates at 5,000 cells per well in DMEM supplemented with 10% FBS. Venetoclax (ABT-199) in the same culture medium is added in half-log dilutions starting at 5μM. The cells are then incubated at 37℃(5% CO2) for 48h, and the effects on proliferation are determined using Cell TiterGlo reagent.

动物实验:

Mice

Nonobese diabetic/severe combined immunodeficient γ (NSG) mice are injected at 6 weeks of age in the tail vein with 150µL phosphate-buffered saline containing 5×106 luciferase-labeled LOUCY cells. At regular time points, the bioluminescence is measured using the IVIS Lumina II imaging system. At 6 weeks, the cells are engrafted and the mice are randomly divided into 2 groups (with an equal number of males and females in both groups), and the treatment is started on day 0. Mice are treated with Venetoclax (ABT-199) 100mg/kg body weight or with vehicle via oral gavage for 4 consecutive days. At days 0,2, and 4 the bioluminescene is measured.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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