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  • ABT-199(货号:A3680)
  • ABT-199(货号:A3680)

    CAS:1257044-40-8
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CAS:
CAS:1257044-40-8

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

 

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