ABT-888(Veliparib)/MX-1,ABT888

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ABT-888(Veliparib)/MX-1,ABT888

ABT-888(Veliparib)/MX-1,ABT888

编号ABP000419 化学名称ABT-888(Veliparib)/MX-1,ABT888 CAS912444-00-9 分子式C13H16N4O 分子量244.2923 纯度 99%

化学名称 : ABT-888(Veliparib)/MX-1,ABT888

CAS : 912444-00-9

英文名称: ABT-888(Veliparib)/MX-1,ABT888

英文同义词: 2-[(2R)-2-methyl-2-pyrrolidinyl]-1H-benzimidazole-7-carboxamide

溶解度:Soluble in water or DMSO

储存条件:-20C 2 years

生物活性

Potent inhibitor of PARP-1 and PARP-2 (potency <5nM in vitro). Does not inhibit other NAD-binding enzymes.Has minimal CYP450 inhibition and induction.Shows broad spectrum of chemo- and radiopotentiation. Enantiomeric purity >97% suitable for in vivo studies. Does not show inherent cytotoxicity and shows no single agent activity in tumor models. Has excellent bioavailability and good blood-brain permeation. Increases tumor growth delay resulting from radiation and DNA-damaging agents.

参考文献

1, Inhibition of poly(ADP-ribose) polymerase enhances cell death and improves tumor growth delay in irradiated lung cancer models: J.M. Albert, et al.; Clin. Cancer Res. 13, 3033 (2007) 2, ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models: C.K. Donawho, et al.; Clin. Cancer Res. 13, 2728 (2007)

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