Information
Iniparib (BSI-201, NSC-746045, IND-71677) is aPARP1inhibitor 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. 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.
In vivo
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：5, and 9 days
Powder Purity:≥99%
| ALogP | 1.3 |
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| Isómeros SMILES | C1=CC(=C(C=C1C(=O)N)[N+](=O)[O-])I |
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| WGK Alemania | 3 |
| Peso molecular | 292.03 |
| Reaxy-Rn | 7704659 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7704659&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubilidad | Solubility (25°C) In vitro DMSO: 62 mg/mL warmed with 50ºC Water: bath (152.14 mM); Ethanol: 2 mg/mL warmed with 50ºC Water: bath (4.9 mM); Water: Insoluble; |
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