化学性质
Storage | Store at -20°C |
M.Wt | 292.03 |
Cas No. | 160003-66-7 |
Formula | C7H5IN2O3 |
Synonyms | BSI201,BSI 201 |
Solubility | insoluble in H2O; ≥103.4 mg/mL in DMSO; ≥24.3 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 4-iodo-3-nitrobenzamide |
Canonical SMILES | C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I |
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。 |
资料参考
Iniparib,原名为BSI-201,是一种静脉注射的PARP1抑制剂,其单独使用或与化学疗法合用在体内外研究中均具有重要的抗肿瘤活性。Iniparib有效对抗各种培养的癌症细胞,包括耐药细胞系。据报道,Iniparib是一种前药,其C-亚硝基代谢物(4-碘-3-硝基苯甲酰胺)通过氧化PARP-1的锌指,使锌游离出来并抑制PARP活性,最终选择性地杀死肿瘤细胞。
参考文献:
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.
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.
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
生物活性
Description | Iniparib(BSI-201)是静脉注射的PARP1抑制剂。 |
靶点 | PARP1 | | | | | |
IC50 | | | | | | |