Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.

Iniparib nonselectively modifies cysteine-containing proteins in tumor cells^[1]. Iniparib (100 μM) weakly inhibits SSB repair, and the inhibition can be reversed by knockdown of PARP1^[2]. Iniparib in combination with cisplatin is cytotoxic to Myc/MDA-231 with EMT changes^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

292.03

C₇H₅IN₂O₃

160003-66-7

Room temperature in continental US; may vary elsewhere.

DMSO : 100 mg/mL (342.43 mM; Need ultrasonic)

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, 6 months; -20°C, 1 month。-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。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.56 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

• [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.

  [4]. 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.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [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.

  [4]. 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.