Iniparib，以前命名為BSI-201，是一種靜脈給藥的PARP1抑制劑，無論是單獨(dú)使用還是與化療聯(lián)合使用，在體外和體內(nèi)研究中都具有重要的抗腫瘤活性。它對多種培養(yǎng)的癌細(xì)胞有活性，包括耐藥細(xì)胞系。據(jù)報道，Iniparib是一種前藥，其C-亞硝基代謝物4-碘-3-亞硝基苯甲酰胺通過氧化PARP-1的鋅指導(dǎo)致鋅排出并抑制PARP活性來選擇性殺死腫瘤細(xì)胞。

產(chǎn)品性質(zhì)：

Cas No.：160003-66-7

別名：3-硝基-4-碘苯甲酰胺,BSI201,BSI 201

化學(xué)名：4-iodo-3-nitrobenzamide

Canonical SMILES：C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I

分子式：C7H5IN2O3

分子量：292.03

溶解度：≥ 103.4 mg/mL in DMSO, ≥ 24.3 mg/mL in EtOH with ultrasonic and warming

儲存條件：Store at -20°C

注意事項(xiàng)：

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References：

[1].Liang H, Tan AR. Iniparib, a PARP1 inhibitor for the potential treatment of cancer, including triple-negative breast cancer. IDrugs. 2010 Sep;13(9):646-56.

[2].Xuesong Liu, Yan Shi, David X. Maag, Joann P. Palma, Melanie J. Patterson, Paul A. Ellis, Bruce W. Surber, Damien B. Ready, Niru B. Soni, Uri S. Ladror, Allison J. Xu, Ramesh Iyer, John E. Harlan, Larry R. Solomon, Cherrie K. Donawho, Thomas D. Penning, Eric F. Johnson, Alexander R. Shoemaker. Iniparib Nonselectively Modifies Cysteine-Containing Proteins in Tumor Cells and Is Not a Bona Fide PARP Inhibitor. Clinical Cancer Research. January 15, 2012 18; 510.

[3].S. Kopetz, M. M. Mita, I. Mok, K. K. Sankhala, J. Moseley, B. M. Sherman, C. R. Bradley and A. W. Tolcher. First in human phase I study of BSI-201, a small molecule inhibitor of poly ADP-ribose polymerase (PARP) in subjects with advanced solid tumors. Journal of Clinical Oncology. (Meeting Abstracts) May 2008 vol. 26 no. 15_suppl 3577