1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP

BSI-201 (Synonyms: Iniparib; NSC-746045; IND-71677)

Cat. No.: HY-12015 Purity: 99.46%
Data Sheet SDS Handling Instructions

BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC).

For research use only. We do not sell to patients.
BSI-201 Chemical Structure

BSI-201 Chemical Structure

CAS No. : 160003-66-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $77 In-stock
10 mg $70 In-stock
50 mg $250 In-stock
100 mg $350 In-stock
200 mg $650 In-stock
500 mg $1500 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

BSI-201 (Iniparib; NSC-746045) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). IC50 Value: Target:PARP1 in vitro: BSI-201 inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. 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. 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. 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.

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01033292 Sanofi Ovarian Cancer December 2009 Phase 2
NCT01033123 Sanofi Ovarian Cancer December 2009 Phase 2
NCT00298675 Sanofi Tumors March 2006 Phase 1
NCT00687765 Sanofi Glioblastoma July 2008 Phase 1|Phase 2
NCT00687687 Sanofi|Gynecologic Oncology Group Uterine Carcinosarcoma May 2008 Phase 2
NCT01551680 Institut du Cancer de Montpellier - Val d'Aurelle Brain Metastases September 2012 Phase 1
NCT00422682 Sanofi Tumors January 2007 Phase 1
NCT01213381 Sanofi Advance Solid Tumors September 2010 Phase 1
NCT00813956 Sanofi|Breast Cancer Research Foundation Triple Negative Breast Cancer December 2008 Phase 2
NCT01204125 Sanofi|SOLTI Breast Cancer Research Group Breast Cancer Female September 2010 Phase 2
NCT01455532 Sanofi Neoplasm Malignant November 2011 Phase 1
NCT01593228 Sanofi Solid Tumors May 2012 Phase 3
NCT01033292 Sanofi Ovarian Cancer December 2009 Phase 2
NCT01033123 Sanofi Ovarian Cancer December 2009 Phase 2
NCT00298675 Sanofi Tumors March 2006 Phase 1
NCT00687765 Sanofi Glioblastoma July 2008 Phase 1|Phase 2
NCT00687687 Sanofi|Gynecologic Oncology Group Uterine Carcinosarcoma May 2008 Phase 2
NCT01551680 Institut du Cancer de Montpellier - Val d'Aurelle Brain Metastases September 2012 Phase 1
NCT00422682 Sanofi Tumors January 2007 Phase 1
NCT01213381 Sanofi Advance Solid Tumors September 2010 Phase 1
NCT00813956 Sanofi|Breast Cancer Research Foundation Triple Negative Breast Cancer December 2008 Phase 2
NCT01204125 Sanofi|SOLTI Breast Cancer Research Group Breast Cancer Female September 2010 Phase 2
NCT01455532 Sanofi Neoplasm Malignant November 2011 Phase 1
NCT01593228 Sanofi Solid Tumors May 2012 Phase 3
NCT01161836 Sanofi Advanced Solid Tumors July 2010 Phase 1
NCT00677079 Sanofi Primary Peritoneal Cancer|Advanced Epithelial Ovarian Cancer June 2008 Phase 2
NCT01173497 Sanofi|UNC Lineberger Comprehensive Cancer Center Estrogen Receptor Negative (ER-Negative) Breast Cancer|Progesterone Receptor Negative (PR-Negative) Breast Cancer|Human Epidermal Growth Factor Receptor 2 Negative (HER2-Negative) Breast Cancer|Brain Metastases July 2010 Phase 2
NCT01130259 Sanofi Breast Cancer
NCT01045304 Sanofi Breast Cancer, Metastatic February 2010 Phase 2
NCT01086254 Sanofi Non-small Cell Lung Cancer Stage IV May 2010 Phase 2
NCT00540358 Sanofi|BiPar Sciences Breast Cancer October 2007 Phase 2
NCT00938652 Sanofi Breast Cancer July 2009 Phase 3
NCT01082549 Sanofi Squamous Cell Lung Cancer March 2010 Phase 3
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References
Molecular Weight

292.03

Formula

C₇H₅IN₂O₃

CAS No.

160003-66-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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BSI-201
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HY-12015
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