Iniparib (BSI-201)

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

Iniparib (BSI-201) Chemical Structure

Molecular Weight(MW): 292.03

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

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 970 In stock
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3 Customer Reviews

  • Immunoblot analysis of PARylation after treatment with various PARP inhibitors.The asterisk indicates a nonspecific band.

    Nat Methods 2013 10(10), 981-4. Iniparib (BSI-201) purchased from Selleck.

    J Exp Clin Cancer Res 2013 32(1), 95 . Iniparib (BSI-201) purchased from Selleck.

  • Representative Western blot analysis and quantification of the mean intensity of the band of IKB phosphorylation (E) and caspase 3 activation (F) in Wt neurons incubated with TWEAK either alone or in combination with the PARP-1 inhibitor BSI-201.

     

     

    Neuroscience 2010 171, 1256–1264. Iniparib (BSI-201) purchased from Selleck.

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Biological Activity

Description Iniparib (BSI-201) 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

Cell Research:[3]
+ Expand
  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 58 mg/mL (198.6 mM)
Ethanol 28 mg/mL (95.88 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 292.03
Formula

C7H5IN2O3

CAS No. 160003-66-7
Storage powder
Synonyms NSC-746045, IND-71677

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01551680 Terminated Brain Metastases Institut du Cancer de Montpellier - Val dAurelle September 2012 Phase 1
NCT01593228 Completed Solid Tumors Sanofi May 2012 Phase 3
NCT01455532 Completed Neoplasm Malignant Sanofi November 2011 Phase 1
NCT01213381 Completed Advance Solid Tumors Sanofi September 2010 Phase 1
NCT01204125 Active, not recruiting Breast Cancer Female Sanofi|SOLTI Breast Cancer Research Group September 2010 Phase 2
NCT01161836 Completed Advanced Solid Tumors Sanofi July 2010 Phase 1

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID