PARP1-IN-8

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PARP1-IN-8 

PARP1-IN-8 (化合物 11c) 是一种有效的可透过血脑屏障的 PARP1 抑制剂，其 IC50 值为 97 nM。PARP1-IN-8 对人肺腺癌上皮细胞系 A549 具有显著的抗增殖活性。

PARP1-IN-8

PARP1-IN-8 Chemical Structure

CAS No. : 836640-15-4

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生物活性

PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549[1].

IC50 & Target

PARP-1

97 nM (IC50)

体外研究
(In Vitro)

PARP1-IN-8 (compound 11c) (0-10 μM, 24-48 h) shows significantly potent anti-proliferative activity against A549 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line: A549, HFF cells[1]
Concentration: 0, 0.1, 1, 10 μM
Incubation Time: 24, 48 h
Result: Showed significantly potent anti-proliferative activity against A549 cells, and didn’t display any significant cytotoxicity on HFF cells[1].

分子量

403.86

Formula

C23H18ClN3O2
CAS 号

836640-15-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (154.76 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4761 mL 12.3805 mL 24.7611 mL
5 mM 0.4952 mL 2.4761 mL 4.9522 mL
10 mM 0.2476 mL 1.2381 mL 2.4761 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.15 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Almahli H, Hadchity E, Jaballah MY, Daher R, Ghabbour HA, Kabil MM, Al-Shakliah NS, Eldehna WM. Development of novel synthesized phthalazinone-based PARP-1 inhibitors with apoptosis inducing mechanism in lung cancer. Bioorg Chem. 2018 Apr;77:443-456.

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