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A-966492

产品编号 T6366 CAS 934162-61-5

别名: 2-[2-氟-4-[(2S)-2-吡咯烷基]苯基]-1H-苯并咪唑-7-甲酰胺

A966492 是一种新型有效的抑制剂，对 PARP1 和 PARP2 的 Ki 分别为 1 nM 和 1.5 nM。

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A-966492, CAS 934162-61-5

规格	价格/CNY	货期
1 mg	￥ 361	现货
5 mg	￥ 895	现货
10 mg	￥ 1,730	现货
25 mg	￥ 2,950	现货
50 mg	￥ 4,270	现货
100 mg	￥ 5,930	现货
1 mL * 10 mM (in DMSO)	￥ 997	现货

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纯度: 98.53%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	A-96649 is a new-type and effective inhibitor. The Ki of A-966492 for PARP1 and PARP2 is 1 nM and 1.5 nM, respectively.
靶点活性	PARP2:1.5 nM(Ki), PARP1:1 nM(ki)
体外活性	A-966492 is one of the most potent PARP inhibitors that displays excellent potency against the PARP-1 enzyme with a Kiof 1 nM and an EC50 of 1 nM in a whole-cell assay. A-966492 significantly enhances the efficacy of TMZ in a dose-dependent manner. In addition, A-966492 is orally bioavailable across multiple species, crosses the blood−brain barrier, and appears to distribute into tumor tissue. A-966492 represents a promising, structurally diverse benzimidazole analogue and is being further characterized preclinically. [1]
体内活性	A-966492 also shows well in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin. Moreover, A-966492 has excellent pharmaceutical properties and has demonstrated in vivo efficacy in preclinical mouse tumor models in combination with TMZ and carboplatin, as well as single agent activity in a BRCA1-deficient MX-1 tumor model. A-966492 is further characterized in Sprague−Dawley rats, beagle dogs, and cynomolgus monkeys, with A-966492 demonstrating oral bioavailabilities of 34−72% and half-lives of 1.7−1.9 hours. In vivo, A-966492 demonstrates significant enhancement of the efficacy of TMZ in a murine B16F10 syngeneic melanoma model, with the A-966492 combination groups showing superior efficacy. [1]
激酶实验	PARP Enzyme Assay: The enzyme assay is conducted in buffer containing 50 mM Tris, pH 8.0, 1 mM dithiothreitol(DTT), and 4 mM MgCl2. PARP reactions contains 1.5 μM [3H]-NAD+ (1.6 μCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Autoreactions utilizing SPA bead-based detection are carried out in 100 μL volumes in white 96-well plates. Reactions are initiated by adding 50 μL of 2X NAD+ substrate mixture to 50 μL of 2× enzyme mixture containing PARP and DNA. These reactions are terminated by the addition of 150 μL of 1.5 mM benzamide (～1 × 103-fold over its IC50). A 170 μL amount of the stopped reaction mixtures is transferred to streptavidin-coated Flash Plates, incubated for 1 hour, and counted using a TopCount microplate scintillation counter. Ki data are determined from inhibition curves at various substrate concentrations.
细胞实验	C41 cells are treated with A-966492 for 30 minutes in a 96-well plate. PARP are activated by damaging DNA with 1 mM Water2 for 10 minutes. Cells are washed with ice-cold phosphate-buffered saline (PBS) once and fixed with prechilled methanol/acetone (7:3) at -20 °C for 10 minutes. After they are air-dried, plates are rehydrated with PBS and blocked using 5% nonfat dry milk in PBS-Tween(0.05%) (blocking solution) for 30 minutes at room temperature. Cells are incubated with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 minutes followed by washing with PBS-Tween20 five times, and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 μg/mL 40,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 minutes. After washing with PBS-Tween20 5 times, analysis is performed using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI. PARP activity (FITC signal) is normalized with cell numbers (DAPI).(Only for Reference)

别名	2-[2-氟-4-[(2S)-2-吡咯烷基]苯基]-1H-苯并咪唑-7-甲酰胺
分子量	324.35
分子式	C18H17FN4O
CAS No.	934162-61-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (185 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0831 mL	15.4154 mL	30.8309 mL	77.0772 mL
	5 mM	0.6166 mL	3.0831 mL	6.1662 mL	15.4154 mL
	10 mM	0.3083 mL	1.5415 mL	3.0831 mL	7.7077 mL
	20 mM	0.1542 mL	0.7708 mL	1.5415 mL	3.8539 mL
	50 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5415 mL
	100 mM	0.0308 mL	0.1542 mL	0.3083 mL	0.7708 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Penning TD, et al. J Med Chem, 2010, 53(8), 3142-53.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

A-966492 934162-61-5 Chromatin/Epigenetic DNA Damage/DNA Repair PARP poly ADP ribose polymerase A966492 A 966492 Inhibitor inhibit 2-[2-氟-4-[(2S)-2-吡咯烷基]苯基]-1H-苯并咪唑-7-甲酰胺 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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A-966492

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

Keywords