Iniparib

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Chemical Structure| 160003-66-7 同义名 : BSI-201;IND-71677;SAR-240550;INO-2BA;NIBA;ND-71677;NSC-746045
CAS号 : 160003-66-7
货号 : A352626
分子式 : C7H5IN2O3
纯度 : 98%
分子量 : 292.031
MDL号 : MFCD11110639
存储条件：

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(359.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PARP1
描述 PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. BSI-201 is a unique PARP1 inhibitor for its little inhibitory potency on PARP enzymatic activity. However, it can target the zinc finger domain and prevents PARP-1 activation by DNA breaks, as well as non-selectively modifies cysteine-containing proteins in tumor cells[1][2]. The addition of DL-buthionine sulfoximine to BSI-201 produced a more significant effect on proliferation in MDA-MB-231 and MDA-MB-436 cells, whereas BSI-201 alone had little effect[2]. A phase II trial of BSI-201 combined with gemcitabine and carboplatin for the treatment of TN breast cancer have been done[3].
作用机制 BSI-201 targets the zinc finger domain and prevents PARP-1 activation by DNA breaks.[1]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01593228 Solid Tumors Phase 3 Completed - -
NCT01455532 Neoplasm Malignant Phase 1 Completed - United States, Arizona ... 展开 >> Investigational Site Number 840002 Scottsdale, Arizona, United States, 85258 United States, California Investigational Site Number 840004 Los Angeles, California, United States, 90048 United States, Georgia Investigational Site Number 840010 Augusta, Georgia, United States, 30912 United States, Missouri Investigational Site Number 840007 St Louis, Missouri, United States, 63110 United States, Ohio Investigational Site Number 840001 Cincinnati, Ohio, United States, 45267-0542 United States, Texas Investigational Site Number 840006 San Antonio, Texas, United States, 78229 收起 <<
NCT00813956 Triple Negative Breast Cancer Phase 2 Completed - United States, California ... 展开 >> Stanford Comprehensive Cancer Center Stanford, California, United States, 94305 United States, Pennsylvania PrECOG Philadelphia, Pennsylvania, United States, 19103 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.12mL

3.42mL

1.71mL

34.24mL

6.85mL

3.42mL
参考文献

[1]Mendeleyev J, Kirsten E, et al. Potential chemotherapeutic activity of 4-iodo-3-nitrobenzamide. Metabolic reduction to the 3-nitroso derivative and induction of cell death in tumor cells in culture. Biochem Pharmacol. 1995 Aug 25;50(5):705-14.

[2]Liu X, Shi Y, 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.

[3]O'Shaughnessy J, Osborne C, et al. Iniparib plus chemotherapy in metastatic triple-negative breast cancer. N Engl J Med. 2011 Jan 20;364(3):205-14.