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Cat. No. Name Size Price Add Cart
KI1259BSI-20110 mg$192
BSI-20150 mg$592
BSI-201200 mg$1712

Chemical Characteristic

Product NameBSI-201
SynonymsIniparib, SAR240550
CAS No.160003-66-7
Molecular Weight 292.03
FormulaC7H5IN2O3
Chemical Name4-iodo-3-nitrobenzamide
SmilesC(=O)(c1cc(c(cc1)I)[N](=O)O)N
Chemical Structure

Biological activities

BSI-201 is an irreversible inhibitor of PARP1. BSI-201 is the prodrug of 4-iodo-3-nitrosobenzamide, an agent that covalently inhibits PARP1 by binding to its first zinc finger under cell-free conditions.[1] BSI-201 (100 µM) inhibits ionizing radiation-induced SSBs repair in human lymphoid cell lines (Raji cancer cells and LCL35 EBV-transformed lymphoblast cells) based on large endogenous Epstein??arr virus (EBV) circular episomes assay, resulting in 55% repair by 2 hours.[2] In human OVCAR-3 ovarian adenocarcinoma xenografts, the combination of BSI-201 and topotecan produces significant antitumor activity and increases the percentage of complete tumor regression compared with topotecan alone.[3] Furthermore, BSI-201 potentiates antitumor effects of carboplatin and gemcitabine in a triple-negative breast cancer cell line.[4]

Protocols

In vitro: BSI-201 is dissolved in DMSO.[2]

References

[1] Mendeleyev J, 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, 50(5): 705-714.
[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, 109(17): 6590-6595.
[3] Valeria Ossovskaya, et al. Activity of BSI-201, a potent Poly(ADP-ribose) polymerase (PARP1) inhibitor, alone and in combination with topotecan in human ovarian xenografts. 99th AACR Annual Meeting. 2008, 4: 12-16.
[4] Underhill C, et al. A review of PARP inhibitors: from bench to bedside. Ann Oncol. 2011, 22(2): 268-279.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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