Niraparib|1038915-60-4|(尼拉帕尼; MK-4827)-陌孚医药/Medlife

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Niraparib (Synonyms: 尼拉帕尼; MK-4827)

目录号: PL08933 纯度: ≥99%

CAS No. :1038915-60-4

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中文名称	Niraparib
中文别名	尼拉帕尼;尼拉帕尼API;2-[4-((3S)-3-哌啶基)苯基]-2H-吲唑-7-甲酰胺;尼拉帕布;尼若帕布;尼拉帕布2-[4-((3S)-3-哌啶基)苯基]-2H-吲唑-7-甲酰胺;MK4827尼拉帕尼;-[4-((3S)-3-哌啶基)苯基]-2H-吲唑-7-甲酰胺;(S)-2-(4-(哌啶-3-基)苯基)-2H-吲唑-7-羧酰胺
英文名称	Niraparib
英文别名	(S)-2-(4-(Piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide;MK4827;MK-4827 (Niraparib);(S)-2-(4-(piperidin-3-yl)phenyl)-2Hindazole-7-carboxamide;2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;MK-4827;Niraparib;2-{4-[(3R)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide;2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide;4-Quinolinamine;7-chloro-N-[(3-chlorophenyl)[4-(1-pyrrolidinylmethyl)phenyl]methyl]-;CHEMBL1094636;Niraparib (USAN);Niraparib [USAN];pound notMK4827 pound not MK 4827;2-[4-((3S)-3-Piperidinyl)phenyl]-2H-indazole-7-carboxamide;EOS-60867;MK4827 (Niraparib);Niraparib (MK-4827);2-[4-(3S)piperidin-3-ylphenyl]-2H-indazol-7-carboxamide;2H-Indazole-7-carboxamide, 2-[4-(3S)-3-piperidinylphenyl]-;MK-4827,(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxaMide;(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carboxamide hydrocholoride;ZEJULA;HMC2H89N35;MK 4827;Niraparib [USAN:INN];2-{4-[(3S)-piperidin-3-yl]phenyl}indazole-7-carboxamide;MK 4827 (Base);Zejula (TN);GTPL8275;M
Cas No.	1038915-60-4
分子式	C₁₉H₂₀N₄O
分子量	320.39
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Niraparib (MK-4827) 是高效的，具有生物口服利用度的 PARP1 和 PARP2 抑制剂，IC₅₀ 分别为 3.8 nM 和 2.1 nM。Niraparib 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 (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC 50 s of 3.8 and 2.1 nM, respectively. Niraparib 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 (MK-4827) inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. MK-4827 inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10-100 nM range. MK-4827 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 (MK-4827) inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM MK-4827 for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib (MK-4827) 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 met

体内研究(In Vivo)

Niraparib (MK-4827) is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib (MK-4827) 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 (MK-4827) 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

Powder -20°C 3 years；4°C 2 years

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 : 25 mg/mL (78.03 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 80°C) (insoluble)配制储备液

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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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