受注:045-509-1970 |
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Synonyms | NSC-746045, IND-71677 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C7H5IN2O3 |
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分子量 | 292.03 | CAS No. | 160003-66-7 | |
Solubility (25°C)* | 体外 | DMSO | 58 mg/mL (198.6 mM) | |
Ethanol | 37 mg/mL (126.69 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | Iniparib (BSI-201, NSC-746045, IND-71677) is a PARP1 inhibitor with demonstrated effectiveness in triple-negative breast cancer (TNBC). Phase 3. |
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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] |
細胞アッセイ | 細胞株 | MDA-MB-231, and MDA-MB-436 |
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濃度 | Dissolved in DMSO, final concentrations ~10 μM | |
反応時間 | 5, and 9 days | |
実験の流れ | 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. |
Data from [Data independently produced by Nat Methods , 2013, 10(10), 981-4]
Data from [J Exp Clin Cancer Res, 2013, 32(1), 95 ]
Data from [Neuroscience, 2010, 171, 1256–1264]
Histone Parylation factor 1 contributes to the inhibition of PARP1 by cancer drugs [ Nat Commun, 2021, 12(1):736] | PubMed: 33531508 |
Synergistic Anti-Tumor Effect of Combining Selective CDK7 and BRD4 Inhibition in Neuroblastoma [ Front Oncol, 2021, 11:773186] | PubMed: 35198433 |
PARP1-cGAS-NF-κB pathway of proinflammatory macrophage activation by extracellular vesicles released during Trypanosoma cruzi infection and Chagas disease. [ PLoS Pathog, 2020, 21;16(4):e1008474] | PubMed: 32315358 |
The PARP inhibitor AZD2281 (Olaparib) induces autophagy/mitophagy in BRCA1 and BRCA2 mutant breast cancer cells. [ Int J Oncol, 2015, 47(1):262-8] | PubMed: 25975349 |
Synergistic Effect of Trabectedin and Olaparib Combination Regimen in Breast Cancer Cell Lines. [ J Breast Cancer, 2015, 18(4):329-38] | PubMed: 26770239 |
Pharmacological Inhibition of Poly(ADP-Ribose) Polymerases Improves Fitness and Mitochondrial Function in Skeletal Muscle. [Pirinen E, et al. Cell Metab, 2014, 19(6):1034-41] | PubMed: 24814482 |
Effect of a poly(ADP-ribose) polymerase-1 inhibitor against esophageal squamous cell carcinoma cell lines [Nasuno T Cancer Sci, 2014, 105(2):202-10] | PubMed: 24219164 |
Cardamonin inhibits angiotensin II-induced vascular smooth muscle cell proliferation and migration by downregulating p38 MAPK, Akt, and ERK phosphorylation. [Shen YJ J Nat Med, 2014, 68(3):623-9] | PubMed: 24595849 |
A proposed screening paradigm for discovery of covalent inhibitor drugs. [ Drug Metab Lett, 2014, 8(1):19-30] | PubMed: 24628405 |
Site-specific characterization of the Asp- and Glu-ADP-ribosylated proteome. [Zhang Y, et al. Nat Methods , 2013, 10(10):981-4] | PubMed: 23955771 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。