Iniparib (BSI-201)

製品コードS1087 バッチS108701

印刷

化学情報

Synonyms

NSC-746045, IND-71677

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₇H₅IN₂O₃

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

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro	Iniparib (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 of this compound plus buthionine sulfoximine (BSO) induces a 95% cell death among 855-2 cells, and displays a similar effect in other human cancer cells. ^[1] It inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. ^[2] Recently it 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 is likely not via inhibition of PARP activity. ^[3] At 100 μM, it 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] It 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. This compound is cytotoxic to a variety of cell lines at concentrations above 40 μM reflecting a mechanism independent of PARP. ^[5]

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.

in vitro

Iniparib (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 of this compound plus buthionine sulfoximine (BSO) induces a 95% cell death among 855-2 cells, and displays a similar effect in other human cancer cells. ^[1] It inhibits the growth of E-ras 20 cells, the effect of which can be augmented 4-fold when BOS is added. ^[2] Recently it 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 is likely not via inhibition of PARP activity. ^[3] At 100 μM, it 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] It 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. This compound is cytotoxic to a variety of cell lines at concentrations above 40 μM reflecting a mechanism independent of PARP. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MDA-MB-231, and MDA-MB-436
	濃度	Dissolved in DMSO, final concentrations ~10 μM
	反応時間	5, and 9 days
	実験の流れ	Iniparib (BSI-201) is exposed to cells at various concentrations for 5 and 9 days in the presence or absence of buthionine sulfoxamide (BSO). After treatment, cell proliferation is measured by CellTiter-Glo assay.

参考

https://pubmed.ncbi.nlm.nih.gov/7669074/
https://pubmed.ncbi.nlm.nih.gov/11853696/
https://pubmed.ncbi.nlm.nih.gov/22128301/

https://pubmed.ncbi.nlm.nih.gov/22493268/
https://pubmed.ncbi.nlm.nih.gov/22291137/

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カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Combining Multiplexed CRISPR/Cas9-Nickase and PARP Inhibitors Efficiently and Precisely Targets Cancer Cells [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2938]	PubMed: 40327605
Coupling cellular drug-target engagement to downstream pharmacology with CeTEAM [ Nat Commun, 2024, 15(1):10347]	PubMed: 39643609
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

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。

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