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
| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
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.
| Targets |
PARP1
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| ln Vivo |
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| 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].
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| Animal Protocol |
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| References |
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| Additional Infomation |
4-iodo-3-nitrobenzamide is a carbonyl compound and an organohalogen compound.
Iniparib is a small molecule iodobenzamide with potential cytotoxic and antineoplastic activities. Although the mechanism of action is unknown, iniparib appears to be cytotoxic in cells with DNA alterations or DNA damage, like that found in tumor cells with mutations in the ataxia telangiectasia mutated (ATM) gene. ATM encodes a serine/threonine protein kinase and mutations of the gene are associated with ataxia telangiectasia and contribute to certain cancers such as T-cell acute lymphoblastic leukemia, B-cell chronic lymphocytic leukemia and B-cell non-Hodgkin lymphomas. |
| Molecular Formula |
C7H5IN2O3
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| Molecular Weight |
292.03
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| Exact Mass |
291.934
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| Elemental Analysis |
C, 28.79; H, 1.73; I, 43.46; N, 9.59; O, 16.44
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| CAS # |
160003-66-7
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| Related CAS # |
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| PubChem CID |
9796068
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| Appearance |
Light yellow to yellow solid powder
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| Density |
2.1±0.1 g/cm3
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| Boiling Point |
344.8±32.0 °C at 760 mmHg
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| Flash Point |
162.3±25.1 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.696
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| LogP |
1.71
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
13
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| Complexity |
228
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| Defined Atom Stereocenter Count |
0
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| SMILES |
IC1C([H])=C([H])C(C(N([H])[H])=O)=C([H])C=1[N+](=O)[O-]
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| InChi Key |
MDOJTZQKHMAPBK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H5IN2O3/c8-5-2-1-4(7(9)11)3-6(5)10(12)13/h1-3H,(H2,9,11)
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| Chemical Name |
4-iodo-3-nitrobenzamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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.
(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.
| 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 |
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