Iniparib (BSI-201) 化学構造
分子量: 292.03

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Quality Control & MSDS

製品説明

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製品の説明

生物活性

製品説明 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
ターゲット
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

プロトコル (参考用のみ)

細胞アッセイ: [3]

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 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)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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 solvent
別名 NSC-746045, IND-71677
溶解度 (25°C) * In vitro DMSO 58 mg/mL (198.6 mM)
エタノール 28 mg/mL (95.88 mM)
<1 mg/mL (<1 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

カスタマーフィードバック (3)


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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.

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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 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)

文献中の引用 (7)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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