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Niraparib hydrochloride

SKU: orb1304290

描述

Niraparib hydrochloride

研究领域

Cell Biology, Epigenetics & Chromatin, Molecular Biology, Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号1038915-64-8
MW356.85
纯度99.90% (May vary between batches)
分子式C19H21ClN4O
SMILESC(N)(=O)C=1C=2C(=CN(N2)C3=CC=C(C=C3)[C@@H]4CCCNC4)C=CC1.Cl
靶点Apoptosis,PARP
溶解性DMSO:50 mg/mL (140.11 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.6 mM);H2O:180 mg/mL (504.41 mM)

生物活性

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靶点 IC50
PARP3:1300 nM|PARP2:2.1 nM|PARP1:3.8nM|PARP4:330 nM|tankyrase 1:570 nM
体内
In cell assays, MK-4827 exhibits inhibitory effects on PARP activity (EC50: 4 nM) and suppresses the proliferation of cancer cells carrying BRCA-1/2 mutations (IC50: 10-100 nM). It effectively inhibits PARP-1/2 (IC50: 3.8/2.1 nM) but shows significantly lower selectivity (over 100-fold) against PARP-3, V-PARP, and tankyrase-1 (IC50: 1300/330/570 nM). In MDA-MB-436 human breast adenocarcinoma cells with a BRCA-1 mutation, MK-4827 has a CC50 of 18 nM; in CAPAN-1 human pancreatic cancer cells with a BRCA-2 deficiency, the CC50 is 90 nM. Normal human prostatic and breast epithelial cells exhibit resistance to MK-4827. This indicates that PARP inhibitors like MK-4827 have selective cytotoxicity in cancer cells with BRCA-1/2 mutations, minimizing the impact on surrounding tissue.
体外
MK-4827 significantly enhances the effectiveness of radiation on human tumor xenografts (whether p53 wild-type or p53 mutant), demonstrating good tolerability in vivo. When used alone, it also exhibits efficacy against BRCA-1 deficient xenograft models.

储存与操作

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储存-20°C
有效期12 months from date of receipt.
免责声明For research use only

别名

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damage, DNA, breast, anti-tumor, Apoptosis, cancer, bioavailable, lung, PARP2, PARP3, PARP1, PARP, MK 4827, MK 4827 Hydrochloride, MK4827, MK-4827, MK-4827 (hydrochloride), MK4827 Hydrochloride, MK-4827 hydrochloride, MK-4827 Hydrochloride, Niraparib hydrochloride, Niraparib Hydrochloride, Niraparib, orally, ovarian, inhibit, Inhibitor, V-PARP, TANK-1, poly ADP ribose polymerase

相似产品

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  • MK-4827 hydrochloride [orb1227084]

    >98% (HPLC)

    1038915-64-8

    356.8492

    C19H21ClN4O

    10 mg, 5 mg, 25 mg, 50 mg, 2 mg, 100 mg, 200 mg, 500 mg, 1 g
质量保证

质量保证

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our 条款与条件和选购指南.

关键属性

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暂无计算属性。

实验方案信息

可选规格

请在下方选择规格

2 mg
¥ 1,040.00
5 mg
¥ 1,300.00
1 ml x 10 mM (in DMSO)
¥ 1,430.00
10 mg
¥ 1,560.00
25 mg
¥ 2,080.00
50 mg
¥ 2,470.00
100 mg
¥ 3,510.00
发货Usually dispatched within 5-10 working days
批量询价