Niraparib hydrochloride|1038915-64-8|(MK-4827 hydrochloride)-陌孚医药/Medlife

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Niraparib hydrochloride (Synonyms: MK-4827 hydrochloride)

目录号: PL08921 纯度: ≥99%

CAS No. :1038915-64-8

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中文名称	Niraparib hydrochloride
中文别名	尼拉帕尼盐酸盐;苯甲酸尼拉帕利;尼拉帕利盐酸盐
英文名称	Niraparib hydrochloride
英文别名	4-Quinolinamine, 7-chloro-N-[3-[[(1,1-dimethylethyl)amino]methyl]-4-fluorophenyl]-;(3S)-3-[4-[7-(aminocarbonyl)-2H-indazol-2-yl]phenyl]piperidinium chloride;(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide,hydrochloride;MK 4827 hydrochloride (MK-4827 hydrochloride,Nihydrochloride,Niraparib);MK-4827 HCl;(3S)-3-{4-[7-(aminocarbonyl)-2H-indazol-2-yl]phenyl}piperidinium chloride;2-(4-((3S)-Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride;2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrochloride;2H-Indazole-7-carboxamide, 2-(4-(3S)-3-piperidinylphenyl)-, hydrochloride (1:1);MK 4827 hydrochloride;Niraparib hydrochloride;SureCN567839;UNII-L4JFC1PHCI;2-[4-(3S)-3-Piperidinylphenyl]-2H-indazole-7-carboxamide hydrochloride (1:1);MK 4827;EOS-62286;MK-4827 (HCl);MK-4827 (hydrochloride);MK-4827, Niraparib HCl salt;Niraparib Tosylate Monohydrate;2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-, hydrochloride (1:1)
Cas No.	1038915-64-8
分子式	C₁₉H₂₀N₄O^.HCl
分子量	356.85
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Niraparib hydrochloride (MK-4827 hydrochloride) 是一种有效的，具有口服活性的 PARP1 和 PARP2 抑制剂，IC₅₀ 值分别为 3.8 nM 和 2.1 nM。Niraparib hydrochloride 抑制 DNA 损伤修复，诱导凋亡 (apoptosis) 并具有抗肿瘤活性。

生物活性

Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC 50 s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity.

性状

Solid

IC50 & Target[1][2]

PARP-2 2.1 nM (IC50) PARP-1 3.8 nM (IC

体外研究(In Vitro)

Niraparib inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. Niraparib inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10?100 nM range. Niraparib displays excellent PARP 1 and 2 inhibition with IC50=3.8 and 2.1 nM, respectively, and in a whole cell assay. To validate that Niraparib inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM Niraparib for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib inhibits PARP within 15 minutes of treatment reaching about 85% inhibition in the A549 cells at 1 h and about 55% inhibition at 1 h for the H1299 cells. has not independently confirmed the accuracy of these methods. They are for refer

体内研究(In Vivo)

Niraparib is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib is characterized by acceptable pharmacokinetics in rats with plasma clearance of 28 (mL/min)/kg, very high volume of distribution (Vd ss =6.9 L/kg), long terminal half-life (t 1/2 =3.4 h), and excellent bioavailability, F = 65%. Niraparib enhances radiation response of p53 mutant Calu-6 tumor in both cases, with the single daily dose of 50 mg/kg being more effective than 25 mg/kg given twice daily. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Jones P, et al. Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85.
[2]. Bridges KA, et al. Niraparib (MK-4827), a novel poly(ADP-Ribose) polymerase inhibitor, radiosensitizes human lung and breast cancer cells. Oncotarget. 2014 Jul 15;5(13):5076-86.

溶解度数据	In Vitro: DMSO : 250 mg/mL (700.57 mM; Need ultrasonic)H₂O : 100 mg/mL (280.23 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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