Iniparib (BSI-201)

Catalog No.S1087 Synonyms: NSC-746045, IND-71677

For research use only.

Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.

Iniparib (BSI-201) Chemical Structure

CAS No. 160003-66-7

Selleck's Iniparib (BSI-201) has been cited by 14 publications

Purity & Quality Control

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Biological Activity

Description Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
Targets
PARP1 [1]
(Cell-free assay)
In vitro

BSI-201 is described as a prodrug of 4-iodo-3-nitrosobenzamide, an agent that covalently inhibits PARP1 by binding to its first zinc finger under cell-free conditions. Treatment of 120 μM BSI-201 plus buthionine sulfoximine (BSO) induces a 95% cell death among 855-2 cells, and displays a similar effect in other human cancer cells. [1] BSI-201 inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. [2] Recently BSI-201 shows no ability to inhibit PARP enzymatic or cellular activity, but can non-selectively modify cysteine-containing proteins in tumor cells, suggesting the mechanism of action for BSI-201 is likely not via inhibition of PARP activity. [3] BSI-201 (100 μM) inhibits ionizing radiation-induced single-strand breaks (SSBs) repair in human lymphoid cell lines based on large endogenous Epstein–Barr virus (EBV) circular episomes assay, resulting in 55% repair by 2 hours, which can be reversed surprisingly by knockdown of PARP1, indicating that the mechanism of inhibition does not involve trapping PARP at SSBs. [4] BSI-201 is not able to selectively kill homologous recombination (HR)-deficient cells between BRCA2-deficient PEO1 and BRCA2-revertant PEO4, or ATM-deficient GM16666 and ATM-restored GM16667 fibroblasts. BSI-201 is cytotoxic to a variety of cell lines at concentrations above 40 μM reflecting a mechanism independent of PARP. [5]

Protocol (from reference)

Cell Research:[3]
  • Cell lines: MDA-MB-231, and MDA-MB-436
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 5, and 9 days
  • Method: Cells are exposed to various concentrations of BSI-201 for 5, and 9 days in the presence or absence of buthionine sulfoxamide (BSO). After treatment, cell proliferation is measured by CellTiter-Glo assay.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 292.03
Formula

C7H5IN2O3

CAS No. 160003-66-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01161836 Completed Drug: Iniparib Advanced Solid Tumors Sanofi July 2010 Phase 1
NCT01033292 Completed Drug: BSI-201 Ovarian Cancer Sanofi December 2009 Phase 2
NCT01033123 Completed Drug: BSI-201 Ovarian Cancer Sanofi December 2009 Phase 2
NCT00687765 Completed Drug: bsi-201 plus temozolomide Glioblastoma Sanofi July 2008 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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