Iniparib (SAR240550; BSI201; NSC746045; IND71677)

Alias:

NSC-746045; IND-71677; BSI-201; BSI201; BSI 201; NSC746045; NSC-746045; NSC 746045; ND-71677; NIBA; INO-2BA; SAR-240550; SAR 240550; SAR240550; IND-71677; IND 71677; IND71677; Iniparib

Cat No.:V0303 Purity: ≥98%

COA Product Data Instructions for use SDS

Iniparib (SAR-240550; BSI-201; NSC-746045; IND-71677) is a novel, potent, and irreversible inhibitor of PARP1 [poly(ADP-ribose) polymerase-1] with potential anticancer activity.

Iniparib (SAR240550; BSI201; NSC746045; IND71677) Chemical Structure CAS No.: 160003-66-7
Product category: PARP

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Iniparib (SAR-240550; BSI-201; NSC-746045; IND-71677) is a novel, potent, and irreversible inhibitor of PARP1 [poly(ADP-ribose) polymerase-1] with potential anticancer activity. It was the first suspected PARP inhibitor to begin phase III clinical trials, but the trials were stopped due to disappointing outcomes. It showed high efficacy and effectiveness in triple-negative breast cancer (TNBC). When used against different types of cancer cells, including drug-resistant cell lines, iniparib exhibits broad-spectrum antiproliferative activity.

Biological Activity I Assay Protocols (From Reference)

Targets

PARP1

ln Vitro

In vitro activity: Iniparib nonselectively alters proteins that contain cysteines in tumor cells[1]. The weak inhibition of SSB repair caused by iniparib (100 μM) can be overcome by knocking down PARP1[2]. Myc/MDA-231 is cytotoxic to iniparib when combined with cisplatin, causing EMT alterations[3].

ln Vivo

N/A

Cell Assay

The nine-day cell proliferation assay involves plating 2000 and 500 cells/well, respectively, in a 96-well plate for MDA-MB-436 and MDA-MB-231 cells. These cells are then treated with veliparib, cmpd-A, cmpd-C, Iniparib or Iniparib-met at 0, 0.0001, 0.01,0.1, 1 or 10 μM for nine days. A 96-well plate containing 1000 and 4000 cells/well, respectively, of MDAMB-231 and MDA-MB-436 cells is used for the five-day cell proliferation assay. The cells are treated with iniparib or iniparib-met at 0.0.1, 0.3, 1, 3, or 10 μM in the presence of 0, 1.8, 3.75, or 7.5 µM BSO for five days. In a 96-well plate, 1000 cells/well of DLD1^+/+ and DLD1^-/- cells are plated. The cells are then treated with TMZ at 0, 0.003, 0.01, 0.03, 0.1, 0.3, or 1 mM in the presence of 0, 0.005, 0.05, 0.5, or 5 µM veliparib or Iniparib for a period of five days. Cell titer glow is performed following treatment[1].

Animal Protocol

N/A

References

[1]. Iniparib nonselectively modifies cysteine-containing proteins in tumor cells and is not a bona fide PARP inhibitor. Clin Cancer Res. 2012 Jan 15;18(2):510-23.

[2]. Myc mediates cancer stem-like cells and EMT changes in triple negative breast cancers cells. PLoS One. 2017 Aug 17;12(8):e0183578.

[3]. Differential effects of poly(ADP-ribose) polymerase inhibition on DNA break repair in human cells are revealed with Epstein-Barr virus. Proc Natl Acad Sci U S A. 2012 Apr 24;109(17):6590-5.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C7H5IN2O3

Molecular Weight

292.03

Exact Mass

291.93

Elemental Analysis

C, 28.79; H, 1.73; I, 43.46; N, 9.59; O, 16.44

CAS #

160003-66-7

Related CAS #

160003-66-7

Appearance

Solid powder

SMILES

C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I

InChi Key

MDOJTZQKHMAPBK-UHFFFAOYSA-N

InChi Code

InChI=1S/C7H5IN2O3/c8-5-2-1-4(7(9)11)3-6(5)10(12)13/h1-3H,(H2,9,11)

Chemical Name

4-iodo-3-nitrobenzamide

Synonyms

NSC-746045; IND-71677; BSI-201; BSI201; BSI 201; NSC746045; NSC-746045; NSC 746045; ND-71677; NIBA; INO-2BA; SAR-240550; SAR 240550; SAR240550; IND-71677; IND 71677; IND71677; Iniparib

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 58~100 mg/mL (198.6~342.4 mM)

Water: <1 mg/mL

Ethanol: ~28 mg/mL (~95.9 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.4243 mL	17.1215 mL	34.2431 mL
	5 mM	0.6849 mL	3.4243 mL	6.8486 mL
	10 mM	0.3424 mL	1.7122 mL	3.4243 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

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
NCT01045304	Completed	Drug: Iniparib Drug: Gemcitabine	Breast Cancer, Metastatic	Sanofi	February 2010	Phase 2
NCT00687687	Completed	Drug: BSI-201 (Iniparib) Drug: carboplatin	Uterine Carcinosarcoma	Sanofi	May 2008	Phase 2

Biological Data

PARP1 depletion does not affect repair, but relieves the inhibition of repair by the PARP inhibitor Iniparib. Proc Natl Acad Sci U S A . 2012 Apr 24;109(17):6590-5.
Myc/MDA-231 cells are sensitive to iniparib plus cisplatin treatment. PLoS One . 2017 Aug 17;12(8):e0183578.

Activity of veliparib, cmpd-A, comp-B, iniparib, and iniparib-met in BRCA-deficient and -proficient cancer cells (A and B) MDA-MB-436 (A; 2,000 cells per well) and MDA-MB-231 (B; 500 cells per well) cells were plated into 96-well culture plates on day 1. Clin Cancer Res . 2012 Jan 15;18(2):510-23.

Veliparib, but not iniparib, inhibits capan-1 xenograft tumor growth as a single agent and potentiates temozolomide in B16F10 xenograft tumors. Clin Cancer Res . 2012 Jan 15;18(2):510-23.