ABT-199

货号：A3680

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。

产品描述

Bcl-2 (B-cell lymphoma 2) is the first identified apoptotic regulator. It belongs to Bcl-2 family commitment to PCD, which regulates apoptosis, pro-apoptosis or anti-apoptosis. ABT-199 is a highly potent inhibitor of Bcl-2, re-engineered from ABT-263. It has subnanomolar affinity (Ki<0.010 nM, analysis by TR–FRET assay), which is over three orders of magnitude to Bcl-XL (Ki=48nM) and Bcl-W (Ki=245 nM). ABT-199 can disrupt BCL-2–BIM complex and induce multiple hallmarks of apoptosis, including cytochrome c release, caspase activation, the externalization of phosphatidylserine and the accumulation of sub-G0/G1 DNA, with lower concentration than ABT-263. Thus it facilitates ABT-199 to have cell-killing activity to Bcl-2 high-expressed NHL cell lines. ABT-199 can inhibit tumor xenograft growth as a single agent or combination with rituximab and bendamustine.

靶点

Bcl-2
Ki:0.01nM

 

作用机制

ABT-199 is complicated by the high degree of similarity within the BH3-binding domains of Bcl-2 and Bcl-XL.

 

储存液制备	质量	1 mg	5 mg	10 mg
	1 mM	1.1515 mL	5.7575 mL	11.5149 mL
	5 mM	0.2303 mL	1.1515 mL	2.3030 mL
	10 mM	0.1151 mL	0.5757 mL	1.1515 mL

  

产品性质

CAS号	1257044-40-8
分子式	C257H383N65O77S6
分子量	868.44
溶解度	DMSO	95.0 mg/mL (109.4 mM) warming
	Water	lnsoluble
	Ethanol	lnsoluble