| CAS NO: | 912445-05-7 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 200mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 317.21 |
| Cas No. | 912445-05-7 |
| Formula | C13H18Cl2N4O |
| Synonyms | ABT-888 dihydrochloride;ABT888 dihydrochloride;ABT 888 dihydrochloride |
| Solubility | ≥31.7 mg/mL in DMSO; ≥104 mg/mL in H2O; ≥3.3 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 2-[(2R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide;dihydrochloride |
| Canonical SMILES | CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N.Cl.Cl |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Veliparib dihydrochloride是一种有效的PARP1和PARP2抑制剂，K(i)值分别为5.2和2.9 nmol/L[1]。
PARP是聚ADP核糖聚合酶的简称，在多种癌症中过表达。由于多种癌症比起正常细胞更不依赖于PARP，使得PARP成为一种引人注目的癌症治疗目标。许多研究表明，PARP抑制剂在临床前研究的体外和体内模型中可作为放疗和化疗增敏剂[2][3]。
Veliparib dihydrochloride是一种PARP的选择性抑制剂。在结肠癌细胞系HCT-116和HT-29中，以veliparib dihydrochloride为佐剂与SN38或Oxall共同使用，可提高G2/M细胞周期停滞，并可通过抑制PARP-1和PARP-2提高DNA损伤水平[4]。
在皮下注射B16F10小鼠黑色素瘤细胞的小鼠模型中，口服剂量为3.1 mg/kg/d~25 mg/kg/d的veliparib dihydrochloride与temozolomide可提高药效，并显著减慢肿瘤发展。在MX-1乳腺癌异种移植模型（BRCA1缺失且BRCA2突变）或HCT-116结肠癌模型中也得到了相似的结果[1]。
参考文献：
[1]. Donawho, C.K., et al., ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models. Clin Cancer Res, 2007. 13(9): p. 2728-37.
[2]. Benafif, S. and M. Hall, An update on PARP inhibitors for the treatment of cancer. Onco Targets Ther, 2015. 8: p. 519-28.
[3]. Guillot, C., et al., PARP inhibition and the radiosensitizing effects of the PARP inhibitor ABT-888 in in vitro hepatocellular carcinoma models. BMC Cancer, 2014. 14: p. 603.
[4]. Davidson, D., et al., The PARP inhibitor ABT-888 synergizes irinotecan
treatment of colon cancer cell lines. Invest New Drugs, 2013. 31(2): p. 461-8.
| Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively. | ||||||
| Targets | PARP1 | PARP2 | ||||
| IC50 | 5.2 nM (Ki) | 2.9 nM (Ki) | ||||
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