Iniparib (BSI-201)

目录号: GC15353纯度: >99.50%同义词: 3-硝基-4-碘苯甲酰胺,BSI201,BSI 201
A PARP1 inhibitor

Iniparib (BSI-201)
Cas No.: 160003-66-7
规格价格库存数量操作
10mg¥546.00现货
1
50mg¥1,659.00现货
1
200mg¥5,072.00现货
1
10mM (in 1mL DMSO)¥357.00现货
1

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产品描述 Description

Iniparib, previously named BSI-201, is an intravenously administered PARP1 inhibitor, which either alone or in combination with chemotherapy, has important antitumor activity in studies in vitro and in vivo. It is active against a broad range of cancer cells in culture, including drug resistant cell lines. Iniparib has been reported to be a prodrug whose C-nitroso metabolite, 4-iodo-3-nitrosobenzamide, selectively kills tumor cells by oxidizing the zinc finger of PARP-1 resulting in ejection of zinc and inhibition of PARP activity.

Reference

[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

实验参考方法 Experimental Reference Method

Cell experiment:

For nine day cell proliferation assay, MDA-MB-436 and MDA-MB-231 cells are plated at 2000 and 500 cells/well respectively in a 96-well plate and treated with veliparib, cmpd-A, cmpd-C, Iniparib or Iniparib-met at 0, 0.0001, 0.01,0.1, 1 or 10 μM for nine days. For five day cell proliferation assay, MDAMB-231 and MDA-MB-436 cells are plated at 1000 and 4000 cells/well respectively in a 96-well plate and treated with Iniparib or Iniparib-met at 0. 0.1, 0.3, 1, 3 or 10 μM in the presence of 0, 1.8, 3.75, or 7.5 µM BSO for 5 days. DLD1+/+ and DLD1-/- cells are plated at 1000 cells/well in a 96-well plate and treated with TMZ at 0, 0.003, 0.01, 0.03, 0.1, 0.3 or 1 mM in the presence of 0, 0.005, 0.05, 0.5, or 5 µM veliparib, or Iniparib for five days. After treatment, cell titer glow is carried out[1].

References:

[1]. Liu X, et al. Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res. 2012 Jan 15;18(2):510-23.
[2]. Ma W, et al. Differential effects of poly(ADP-ribose) polymerase inhibition on DNA break repair in human cells are revealed with Epstein-Barr virus. Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6590-5.
[3]. Yin S, et al. Myc mediates cancer stem-like cells and EMT changes in triple negative breast cancers cells. PLoS One. 2017 Aug 17;12(8):e0183578.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
160003-66-7
同义词
3-硝基-4-碘苯甲酰胺,BSI201,BSI 201
化学名
4-iodo-3-nitrobenzamide
SMILES
C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I
分子式
C7H5IN2O3
分子量
292.03 g/mol
溶解性
≥ 103.4 mg/mL in DMSO, ≥ 24.3 mg/mL in EtOH with ultrasonic and warming
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol