ABT-888，也稱為Veliparib，是聚(ADP-核糖)聚合酶(PARP)抑制劑，并在與多種細胞毒性劑組合的廣譜臨床前腫瘤模型中顯示出優(yōu)異的體內(nèi)功效。PARP參與DNA修復，PARP水平升高會導致對細胞毒性化療和放療的抗性。因此，PARP抑制劑有希望成為化療和放射增敏劑。與微衛(wèi)星穩(wěn)定(MSS)細胞系(兩種基因的野生型)相比，ABT-888對含有MRE11和RAD50基因突變的微衛(wèi)星不穩(wěn)定(MSI)細胞系也有活性。

產(chǎn)品性質(zhì)：

Cas No.：912444-00-9

別名：維利帕尼; ABT-888

化學名： 1-[3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]prop-2-en-1-one

Canonical SMILES CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N

分子式：C13H16N4O

分子量：244.3

溶解度：≥ 6.1mg/mL in DMSO

儲存條件：Store at -20°C

注意事項：

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References：

1、Shivaani Kummar, Robert Kinders, Martin E. Gutierrez, Larry Rubinstein, Ralph E. Parchment, Lawrence R. Phillips, Jiuping Ji, Anne Monks, Jennifer A. Low, Alice Chen, Anthony J. Murgo, Jerry Collins, Seth M. Steinberg, Helen Eliopoulos, Vincent L. Giranda, Gary Gordon, Lee Helman, Robert Wiltrout, Joseph E. Tomaszewski and James H. Doroshow. Phase 0 Clinical Trial of the Poly (ADP-Ribose) Polymerase Inhibitor ABT-888 in Patients With Advanced Malignancies. Journal of Clinical Oncology. 2009; 27(16): 2705 – 11.

2、Xiaofeng Li, Juergen Delzer, Richard Voorman, Sonia M. de Morais and Yanbin Lao. Disposition and Drug-Drug Interaction Potential of Veliparib (ABT-888), a Novel and Potent Inhibitor of Poly (ADP-ribose) Polymerase. DRUG METABOLISM AND DISPOSITION. 2011; 39(7): 1161 – 69.

3、E. Vilar Sanchez, A. Chow, L. Raskin, M. D. Iniesta, B. Mukherjee and S. B. Gruber. Preclinical testing of the PARP inhibitor ABT-888 in microsatellite instable colorectal cancer. Journal of Clinical Oncology. 2009; 27(15S): 11028A.