Iniparib (BSI-201)

BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.

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Iniparib (BSI-201) Chemical Structure

Iniparib (BSI-201) Chemical Structure
Molecular Weight: 292.03

Validation & Quality Control

Customer Reviews(3)

Quality Control & MSDS

Related Compound Libraries

Iniparib (BSI-201) is available in the following compound libraries:

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Product Information

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  • Research Area

Product Description

Biological Activity

Description BSI-201 (Iniparib, SAR240550) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3.
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]
In vivo
Features

Protocol(Only for Reference)

Cell Assay: [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.
1

References

[1] Mendeleyev J, et al. Biochem Pharmacol, 1995, 50(5), 705-714.

[2] Bauer PI, et al. Biochem Pharmacol, 2002, 63(3), 455-462.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01213381 Completed Advance Solid Tumors Sanofi 2010-09 Phase 1
NCT01204125 Active, not recruiting Breast Cancer Female Sanofi|SOLTI Breast Cancer Research Group 2010-09 Phase 2
NCT01455532 Active, not recruiting Neoplasm Malignant Sanofi 2011-11 Phase 1
NCT01593228 Recruiting Solid Tumors Sanofi 2012-05 Phase 3
NCT01551680 Recruiting Brain Metastases Centre Val d'Aurelle - Paul Lamarque 2012-09 Phase 1

Chemical Information

Download Iniparib (BSI-201) SDF
Molecular Weight (MW) 292.03
Formula

C7H5IN2O3

CAS No. 160003-66-7
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms NSC-746045, IND-71677
Solubility (25°C) * In vitro DMSO 58 mg/mL (198 mM)
Water <1 mg/mL (<1 mM)
Ethanol 28 mg/mL (95 mM)
* <1 mg/ml means slightly soluble or 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 Name 4-iodo-3-nitrobenzamide

Research Area

Customer Reviews (3)


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Rating
Source J Exp Clin Cancer Res, 2013, 32(1):95 . Iniparib (BSI-201) purchased from Selleck
Method flow cytometry
Cell Lines MCF7-ATMi and MCF7 cells
Concentrations 0-5 uM
Incubation Time 48 h
Results MCF7-ATMi cells are more sensitive than MCF7-ctr cells to iniparib

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Rating
Source Nat Methods, 2013, 10(10):981-4. Iniparib (BSI-201) purchased from Selleck
Method Immunoblot analysis
Cell Lines HCT116
Concentrations 50 uM
Incubation Time 40 min
Results Immunoblot analysis of PARylation after treatment with AIniparib.The asterisk indicates a nonspecific band.

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Rating
Source Neuroscience 2010 171, 1256–1264. Iniparib (BSI-201) purchased from Selleck
Method Western blot
Cell Lines Wt neurons
Concentrations 25 μM
Incubation Time 24 h
Results Our results indicate that TWEAK induces NF-κB activation in neurons and that this effect is abrogated by PARP-1 inhibitor BSI-201 (Fig. E). Wt neurons were incubated with TWEAK alone or in combination with BSI-201 followed by a Western blot analysis with an antibody that detects cleaved caspase-3. We found that TWEAK induces caspase-3 cleavage and that this effect is attenuated by PARP-1 inhibitor BSI-201 (Fig. F)

Product Citations (5)

Tech Support & FAQs

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