Iniparib (BSI-201)

Catalog No.S1087

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

Price Stock Quantity  
USD 160 In stock
USD 120 In stock
USD 370 In stock
USD 970 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Iniparib (BSI-201) Chemical Structure

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

Validation & Quality Control

3 customer reviews :

Quality Control & MSDS

Related Compound Libraries

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

PARP Inhibitors with Unique Features

  • Pan PARP Inhibitors

    Olaparib (AZD2281, Ku-0059436) Pan-PARP1/2 inhibitor, IC50=5 nM/1 nM.

  • Most Potent PARP Inhibitor

    MK-4827 (Niraparib) PARP1, IC50=3.8 nM; PARP2, IC50=2.1 nM.

  • PARP Inhibitor in Clinical Trial

    Veliparib (ABT-888) Phase III for solid tumors.

  • Newest PARP Inhibitor

    BMN 673 Novel?b>PARP爄nhibitor with?b>IC50爋f 0.58 nM. Also a potent inhibitor of PARP-2, but does not inhibit PARG and highly sensitive to PTEN mutation.

Product Information

  • Compare PARP Inhibitors
    Compare PARP Products
  • Research Area

Product Description

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]
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
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.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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 Active, not recruiting 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

view more

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 solvent
Synonyms NSC-746045, IND-71677
Solubility (25°C) * In vitro DMSO 58 mg/mL (198.6 mM)
Ethanol 28 mg/mL (95.88 mM)
Water <1 mg/mL (<1 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

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related PARP Products

  • G007-LK

    G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.

  • NU1025

    NU1025 is a potent PARP inhibitor with IC50 of 400 nM.

  • SCR7

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).

  • Olaparib (AZD2281, Ku-0059436)

    Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Phase 3.

    Features:A potent PARP inhibitor (currently in late stage clinical trials).

  • Veliparib (ABT-888)

    Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Phase 3.

    Features:Increases the efficacy of common cancer therapies such as radiation and alkylating agents.

  • Rucaparib (AG-014699,PF-01367338)

    Rucaparib (AG-014699, PF-01367338) is an inhibitor of PARP with Ki of 1.4 nM for PARP1 in a cell-free assay, also showing binding affinity to eight other PARP domains. Phase 3.

    Features:The first PARP inhibitor used in clinical trials combined with temozolomide.

  • Talazoparib (BMN 673)

    Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.

    Features:Most potent and selective PARPi reported thus far.

  • PJ34 HCl

    PJ34 HCl is the hydrochloride salt of PJ34, which is a PARP inhibitor with EC50 of 20 nM and is equally potent to PARP1/2.

    Features:Water-soluble PARP1/2 inhibitor with >10,000-fold potentcy vs. 3-aminobenzamide (prototypical PARP inhibitor). Potential uses in cardiovascular diseases (stroke, cerebral ischemia, & myocardial ischemia).

  • AG-14361

    AG14361 is a potent inhibitor of PARP1 with Ki of <5 nM in a cell-free assay. It is at least 1000-fold more potent than the benzamides.

    Features:The 1st high-potency PARP-1 inhibitor with the specificity & in vivo activity to enhance chemotherapy and radiation therapy of human cancers.

  • A-966492

    A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.

    Features:A promising, structurally diverse benzimidazole analogue that is being further characterized preclinically.

Recently Viewed Items

Tags: buy Iniparib (BSI-201) | Iniparib (BSI-201) supplier | purchase Iniparib (BSI-201) | Iniparib (BSI-201) cost | Iniparib (BSI-201) manufacturer | order Iniparib (BSI-201) | Iniparib (BSI-201) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us