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抑制剂/激动剂
细胞生物学 肿瘤
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/ Iniparib

3-硝基-4-碘苯甲酰胺 /Iniparib {[allProObj[0].p_purity_real_show]}

货号：A352626 同义名： BSI-201;IND-71677

Iniparib是一种PARP1抑制剂，已证明在三阴性乳腺癌（TNBC）中具有疗效。

Iniparib 化学结构 CAS号：160003-66-7
Iniparib 化学结构
CAS号：160003-66-7
Iniparib 3D分子结构
CAS号：160003-66-7
Iniparib 化学结构 CAS号：160003-66-7
Iniparib 3D分子结构 CAS号：160003-66-7
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Iniparib 纯度/质量文件 产品仅供科研

货号：A352626 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 PARP ↓ PARP1 ↓ PARP2 ↓ PARP3 ↓ 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

 		99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

 		99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

 		98%
AZD-2461 ✔ 99%+
BGP-15 ✔ 99%+
NU1025 +

PARP, IC50: 400 nM

 		97%
Benzamide +

PARP, IC50: 3.3 μM

 		98%
Picolinamide +

PARP, IC50: 95 μM

 		98%
AG14361 +++

PARP1, Ki: <5 nM

 		98+%
Iniparib ✔ 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

 		99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

 		98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

 		++

PARP2, IC50: 0.3 μM

 		98%
A-966492 ++++

PARP1, Ki: 1 nM

PARP1, EC50: 1 nM

 		+++

PARP2, Ki: 1.5 nM

 		99%+
Veliparib ++

PARP1, Ki: 5.2 nM

 		+++

PARP2, Ki: 2.9 nM

 		98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		99%+
Stenoparib ++++

PARP1, IC50: 1 nM

 		++++

PARP2, IC50: 1.2 nM

 		98%
Olaparib +++

PARP1, IC50: 5 nM

 		++++

PARP2, IC50: 1 nM

 		98%
Niraparib +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		98%
ME0328 +

PARP1, IC50: 6.3 μM

 		+

PARP3, IC50: 0.89 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Iniparib 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]

Iniparib 动物研究

Dose Hamster: 200 mg/kg[1] (i.p.)
Administration i.p.

Iniparib 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 <<

Iniparib 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.

Iniparib 实验方案

计算器
存储液制备 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

Iniparib 技术信息

CAS号160003-66-7
分子式C7H5IN2O3
分子量 292.031
别名 BSI-201;IND-71677;SAR-240550;INO-2BA;NIBA;ND-71677;NSC-746045
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

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

Tags: Iniparib | 160003-66-7 | BSI-201 | NSC-746045 | IND-71677 | BSI201 | BSI 201 | NSC746045 | NSC 746045 | NSC-746045 | IND71677 | IND 71677 | IND-71677 | PARP Inhibitor | Cell Cycle/DNA Damage | Epigenetics | Anti-infection | PARP | Influenza Virus | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Iniparib 纯度/质量文件 | Iniparib 亚型比较 | Iniparib 生物活性 | Iniparib 动物研究 | Iniparib 临床数据 | Iniparib 参考文献 | Iniparib 实验方案 | Iniparib 技术信息

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