Iniparib (BSI-201) 化学構造
分子量: 292.03

品質と確認

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Quality Control & MSDS

製品情報

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    PARP阻害剤を比較
  • 研究分野

製品の説明

生物活性

情報 Iniparib (BSI-201)は、推定のPoly(ADPリボース)ポリメラーゼ(PARP I)阻害剤です
目標
IC50
In vitro試験 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]
In vivo試験
臨床試験
特集

推薦された実験操作 (公開の文献だけ)

細胞アッセイ: [3]

細胞系 MDA-MB-231, and MDA-MB-436
濃度 Dissolved in DMSO, final concentrations ~10 μM
処理時間 5, and 9 days
方法 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Iniparib (BSI-201) SDF
分子量 292.03
化学式

C7H5IN2O3

CAS No. 160003-66-7
保管 2年-20℃
6月-80℃in DMSO
別名 NSC-746045, IND-71677
溶解度 (25°C) * In vitro DMSO 58 mg/mL (198 mM)
<1 mg/mL (<1 mM)
エタノール 28 mg/mL (95 mM)
* <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.
化学名 4-iodo-3-nitrobenzamide

研究分野

カスタマーレビュー (3)


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Rating
Source Neuroscience, 2010, 171, 1256–1264. Iniparib (BSI-201) purchased from Selleck
Method Western blot
Cell Lines Wt neurons
Concentrations 25 μM
Incubation Time 24 h
Results Our results indicate that TWEAK induces NF-κB activation in neurons and that this effect is abrogated by PARP-1 inhibitor BSI-201 (Fig. E). Wt neurons were incubated with TWEAK alone or in combination with BSI-201 followed by a Western blot analysis with an antibody that detects cleaved caspase-3. We found that TWEAK induces caspase-3 cleavage and that this effect is attenuated by PARP-1 inhibitor BSI-201 (Fig. F)

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Rating
Source , , J Exp Clin Cancer Res, 2013, 32(1):95 . Iniparib (BSI-201) purchased from Selleck
Method flow cytometry
Cell Lines MCF7-ATMi and MCF7 cells
Concentrations 0-5 uM
Incubation Time 48 h
Results MCF7-ATMi cells are more sensitive than MCF7-ctr cells to iniparib

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Rating
Source , , Nat Methods, 2013, 10(10):981-4. Iniparib (BSI-201) purchased from Selleck
Method Immunoblot analysis
Cell Lines HCT116
Concentrations 50 uM
Incubation Time 40 min
Results Immunoblot analysis of PARylation after treatment with AIniparib.The asterisk indicates a nonspecific band.

製品表彰状 (6)

技術サポート&よくある質問(FAQ)

顧客がするかもしれない質問に対する答えは、指示を取り扱っている阻害剤で見つかります。話題は、貯蔵液(阻害剤と特別な注意を細胞ベースの分析法と動物のために必要とする問題を保存することは実験します)を準備する方法を含みます。

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