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/ Iniparib

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。BSI-201与其他小分子联合使用时，使得能够从人类和小鼠衍生扩展多能干细胞 (EPS)。

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
规格 价格 会员价 库存 数量
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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

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
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

 		98%
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

 		97%
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 细胞实验

Cell Line
Concentration Treated Time Description References
LCL35 cells 100 µM 2 hours Evaluate the effect of Iniparib on the repair of radiation-induced single-strand breaks, showing that Iniparib inhibited SSB repair, but PARP1 knockdown reversed this inhibition Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6590-5.
Raji cells 100 µM 2 hours Evaluate the effect of Iniparib on the repair of radiation-induced single-strand breaks, showing that Iniparib inhibited SSB repair Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6590-5.
HepG2 cells 10, 20, 40, 60, 80 µM 24, 48, 72, 96 hours BSI-201 inhibited the proliferation of HepG2 cells in a time- and concentration-dependent manner. Mol Med Rep. 2017 Jul;16(1):208-214.
HepG2 cells 50, 100, 200, 400, 800 µM 24, 48, 72, 96 hours AZD2281 inhibited the proliferation of HepG2 cells in a time- and concentration-dependent manner. Mol Med Rep. 2017 Jul;16(1):208-214.
HepG2 cells 5, 10, 20, 40, 80 µM 24, 48, 72, 96 hours AG014699 inhibited the proliferation of HepG2 cells in a time- and concentration-dependent manner. Mol Med Rep. 2017 Jul;16(1):208-214.
HCC-1428 2 µM 4 days Evaluate the effects of PARP inhibitors on BRCA mutant cell lines, BSI-201 did not induce cell death at 2 µM Int J Oncol. 2015 Jul;47(1):262-8.
SUM-149PT 2 µM 4 days Evaluate the effects of PARP inhibitors on BRCA mutant cell lines, BSI-201 did not induce cell death at 2 µM Int J Oncol. 2015 Jul;47(1):262-8.
MDA-MB-436 2 µM 4 days Evaluate the effects of PARP inhibitors on BRCA mutant cell lines, BSI-201 did not induce cell death at 2 µM Int J Oncol. 2015 Jul;47(1):262-8.
HCC-1937 2 µM 4 days Evaluate the effects of PARP inhibitors on BRCA mutant cell lines, BSI-201 did not induce cell death at 2 µM Int J Oncol. 2015 Jul;47(1):262-8.
MDA-MB-231 50 µM 48 hours To evaluate the therapeutic effect of Iniparib on MDA-MB-231 cells, results showed sensitivity to iniparib plus cisplatin but resistance to iniparib alone, cisplatin, paclitaxel, and docetaxel. PLoS One. 2017 Aug 17;12(8):e0183578.
MDA-MB-468 50 µM 48 hours To evaluate the therapeutic effect of Iniparib on MDA-MB-468 cells, results showed resistance to iniparib plus cisplatin, iniparib alone, cisplatin, paclitaxel, and docetaxel. PLoS One. 2017 Aug 17;12(8):e0183578.
Human NDUFS1 mutant fibroblasts 100 nM 48 hours MRL-45696 increased NAD+ levels and oxygen consumption rate, improving mitochondrial function Cell Metab. 2014 Jun 3;19(6):1034-41.
MCF-7 cells 50 µM 48 hours To evaluate the effect of ATM-depletion on MCF-7 cell sensitivity to iniparib, results showed G2/M phase accumulation. J Exp Clin Cancer Res. 2013 Nov 19;32(1):95.
GM16667 human fibroblasts 80 µM 6 days Evaluate the selective cytotoxicity of Iniparib in ATM-proficient cells, results showed Iniparib had low selectivity for GM16667 cells Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
GM16666 human fibroblasts 80 µM 6 days Evaluate the selective cytotoxicity of Iniparib in ATM-deficient cells, results showed Iniparib had low selectivity for GM16666 cells Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
PEO4 human ovarian cancer cells 80 µM 6 days Evaluate the selective cytotoxicity of Iniparib in HR-proficient cells, results showed Iniparib had low selectivity for PEO4 cells Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
PEO1 human ovarian cancer cells 80 µM 6 days Evaluate the selective cytotoxicity of Iniparib in HR-deficient cells, results showed Iniparib had low selectivity for PEO1 cells Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
Primary myotubes from obese patients 10 nM 72 hours MRL-45696 increased NAD+ levels and oxygen consumption rate, improving mitochondrial function Cell Metab. 2014 Jun 3;19(6):1034-41.
ZR-75-1 cells 100 µM 72 hours To evaluate the effect of ATM-depletion on ZR-75-1 cell sensitivity to iniparib, results showed no effect of ATM-depletion on sensitivity. J Exp Clin Cancer Res. 2013 Nov 19;32(1):95.
SKOV3 human ovarian cancer cells 10 µM continuously Evaluate the sensitization effect of Iniparib to topoisomerase I poisons, results showed Iniparib failed to sensitize SKOV3 cells to topotecan Clin Cancer Res. 2012 Mar 15;18(6):1655-62.
C2C12 myotubes 1–10 nM MRL-45696 reduced redox potential, increased mitochondrial membrane potential and oxygen consumption rate Cell Metab. 2014 Jun 3;19(6):1034-41.

Iniparib 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice SCC1 (head and neck cancer) or MDA-MB-231 (triple-negative breast cancer) xenografts Intraperitoneal injection 50 mg/kg Single dose To evaluate the effect of iniparib on PARP activity. Results showed that iniparib had no significant effect on PARP activity and had a less marked effect on reducing 18F-FTT uptake compared to olaparib. Radiology. 2017 Feb;282(2):453-463
Mice High-fat diet-induced obesity model Dietary admixture 50 mg/kg/day Once daily for 18 weeks MRL-45696 reduced high-fat diet-induced weight gain and fat accumulation, increased energy expenditure, and improved mitochondrial function Cell Metab. 2014 Jun 3;19(6):1034-41.

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 292.03
SMILES Code IC1=C(C=C(C(=O)N)C=C1)[N+](=O)[O-]
MDL No. MFCD11110639
别名 BSI-201; IND-71677; SAR-240550; INO-2BA; NIBA; ND-71677; NSC-746045
运输蓝冰
InChI Key MDOJTZQKHMAPBK-UHFFFAOYSA-N
Pubchem ID 9796068
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二

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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