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/ PARP / Niraparib/尼拉帕尼

Niraparib/尼拉帕尼 {[allProObj[0].p_purity_real_show]}

货号：A298513 同义名： MK-4827( 尼拉帕尼) / MK-4827

Niraparib（MK-4827）是一种高效、口服生物利用度的PARP1和PARP2抑制剂，其IC50分别为3.8 nM和2.1 nM。尼拉帕尼抑制DNA损伤修复，激活凋亡，并显示出抗肿瘤活性。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Niraparib/尼拉帕尼 化学结构 CAS号：1038915-60-4
Niraparib/尼拉帕尼 化学结构
CAS号：1038915-60-4
Niraparib/尼拉帕尼 3D分子结构
CAS号：1038915-60-4
Niraparib/尼拉帕尼 化学结构 CAS号：1038915-60-4
Niraparib/尼拉帕尼 3D分子结构 CAS号：1038915-60-4
规格 价格 会员价 库存 数量
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Niraparib/尼拉帕尼 纯度/质量文件 产品仅供科研

货号：A298513 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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产品名称 PARP ↓ PARP1 ↓ PARP2 ↓ PARP3 ↓ 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

 		99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

 		99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

 		98%
AZD-2461 ✔ 99%+
BGP-15 ✔ 99%+
NU1025 +

PARP, IC50: 400 nM

 		98%
Benzamide +

PARP, IC50: 3.3 μM

 		98%
Picolinamide +

PARP, IC50: 95 μM

 		98%
AG14361 +++

PARP1, Ki: <5 nM

 		98+%
Iniparib ✔ 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

 		99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

 		97%
UPF 1069 +

PARP1, IC50: 8.0 μM

 		++

PARP2, IC50: 0.3 μM

 		98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

 		+++

PARP2, Ki: 1.5 nM

 		99%+
Veliparib ++

PARP1, Ki: 5.2 nM

 		+++

PARP2, Ki: 2.9 nM

 		98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		99%+
Stenoparib ++++

PARP1, IC50: 1 nM

 		++++

PARP2, IC50: 1.2 nM

 		98%
Olaparib +++

PARP1, IC50: 5 nM

 		++++

PARP2, IC50: 1 nM

 		98%
Niraparib +++

PARP1, IC50: 3.8 nM

 		+++

PARP2, IC50: 2.1 nM

 		98%
ME0328 +

PARP1, IC50: 6.3 μM

 		+

PARP3, IC50: 0.89 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Niraparib/尼拉帕尼 生物活性

靶点

  • PARP1

    PARP1, IC50:3.8 nM

  • PARP2

    PARP2, IC50:2.1 nM
描述 PARP1, also called as Poly(ADP-ribose) polymerase, is involved in the signaling of DNA damage. It can recognize and bind DNA single or double-strand breaks, thus possessing various cellular function, including regulation of apoptosis and chromosome stability, gene amplification and transcription, as well as cell division and differentiation. PARP-2 is the closest homolog of PARP1 (~62% similarity in catalytic domain) and compensates for PARP-1 activity in DNA single-strand break. MK-4827 is potent inhibitor of PARP1 and PARP2 with IC50 values of 3.8nM and 2.1nM (measured by PARP isoform TCA assays), respectively, at least a 100-fold selectivity over PARP-3, V-PARP, and tankyrase-1. MK-4827 inhibited PARP activity with EC50 of 4nM and preferentially suppressed proliferation of MDA-MB-436 cells carrying BRCA-1 mutation with CC50 value of 18nM and CAPAN-1 cells carrying BRCA-2 mutantation with CC50 value of 90nM. Oral treatment with MK-4827 at either 100 mg/kg q.d. or 50 mg/kg b.i.d. for 33 days repressed tumor growth in a BRCA-1 mutant MDA-MB-436 xenograft model[1].Oral administration of MK-4827 at a dose of 50mg/kg once daily radiosensitized all four tumors regardless of the p53 status, including Calu-6, H460, A549 and MDA-MB-231, with reduced PAR levels in tumors[2].
作用机制 MK-4827 is a nicotinamide derivate, which can compete with NAD+ for the PARP catalytic site.[3]

Niraparib/尼拉帕尼 细胞实验

Cell Line
Concentration Treated Time Description References
PEO1 cells 10 µM 24 hours Assessed γ-H2AX expression, showing significant increase in DNA damage with combination therapy Research (Wash D C). 2024 May 24;7:0371
A2780 cells 10 µM 24 hours Assessed γ-H2AX expression, showing significant increase in DNA damage with combination therapy Research (Wash D C). 2024 May 24;7:0371
SKOV3 cells 10 µM 24 hours Assessed γ-H2AX expression, showing significant increase in DNA damage with combination therapy Research (Wash D C). 2024 May 24;7:0371
OVCAR3 cells 10 µM 24 hours Assessed γ-H2AX expression, showing significant increase in DNA damage with combination therapy Research (Wash D C). 2024 May 24;7:0371
PEO1 10 µM 48 hours P4 significantly enhanced the growth inhibitory effect of niraparib on PEO1 cells and reduced the IC50 value Research (Wash D C). 2024 May 24;7:0371
A2780 10 µM 48 hours P4 significantly enhanced the growth inhibitory effect of niraparib on A2780 cells and reduced the IC50 value Research (Wash D C). 2024 May 24;7:0371
SKOV3 10 µM 48 hours P4 significantly enhanced the growth inhibitory effect of niraparib on SKOV3 cells and reduced the IC50 value Research (Wash D C). 2024 May 24;7:0371
OVCAR3 10 µM 48 hours P4 significantly enhanced the growth inhibitory effect of niraparib on OVCAR3 cells and reduced the IC50 value Research (Wash D C). 2024 May 24;7:0371
ID8 35 μM 48 h To study the growth inhibition and sensitivity of Niraparib on ID8 cells Mol Cancer Ther. 2025 Mar 4;24(3):453-463.
SKOV3 10 μM 72 h To evaluate the anti-tumor effect of Niraparib on SKOV3 cells, results showed that Niraparib significantly inhibited cell viability. Redox Biol. 2025 Mar;80:103528.
OV90 10 μM 72 h To evaluate the anti-tumor effect of Niraparib on OV90 cells, results showed that Niraparib significantly inhibited cell viability. Redox Biol. 2025 Mar;80:103528.
A2780 10 μM 72 h To evaluate the anti-tumor effect of Niraparib on A2780 cells, results showed that Niraparib significantly inhibited cell viability. Redox Biol. 2025 Mar;80:103528.
OVCAR8 10 μM 72 h To evaluate the anti-tumor effect of Niraparib on OVCAR8 cells, results showed that Niraparib significantly inhibited cell viability. Redox Biol. 2025 Mar;80:103528.
A549-RB1-KO 1 μM 72 h A549-RB1-KO cells showed significantly reduced viability after Niraparib treatment, indicating that RB1 deficiency enhances the effect of PARP inhibitors on DNA damage. JCI Insight. 2023 Nov 8;8(21):e165268.
A549 1 μM 72 h A549 cells formed more colonies after Niraparib treatment, indicating that RB1 wild-type cells are less sensitive to PARP inhibitors. JCI Insight. 2023 Nov 8;8(21):e165268.
H2228 1 μM 72 h H2228 cells formed fewer colonies after Niraparib treatment, indicating that RB1 mutation increased sensitivity to PARP inhibitors. JCI Insight. 2023 Nov 8;8(21):e165268.
UWB1.289 10 μM 48 h To investigate the effect of Niraparib on PD-L1 expression, results showed that Niraparib upregulated PD-L1 expression. J Transl Med. 2021 Oct 7;19(1):415.
SKOV3 10 μM 48 h To investigate the effect of Niraparib on PD-L1 expression, results showed that Niraparib upregulated PD-L1 expression. J Transl Med. 2021 Oct 7;19(1):415.
LLC PARhigh cells 3 to 12 µM 7 days PARhigh LLC cells died after niraparib treatment, while PARP1KO LLC cells showed only a marginal response at the highest dose (12 µM) J Immunother Cancer. 2022 Jun;10(6):e004280.
HO8910 10 μM 48 h To evaluate the apoptotic effect of Niraparib combined with berberine on ovarian cancer cells, the results showed that the combination significantly increased apoptosis. Cell Death Dis. 2017 Oct 5;8(10):e3070.
A2780 10 μM 48 h To evaluate the apoptotic effect of Niraparib combined with berberine on ovarian cancer cells, the results showed that the combination significantly increased apoptosis. Cell Death Dis. 2017 Oct 5;8(10):e3070.
OVCAR3 45 μM 48 h To study the growth inhibition and sensitivity of Niraparib on OVCAR3 cells Mol Cancer Ther. 2025 Mar 4;24(3):453-463.
A2780 80 μM 48 h To study the growth inhibition and sensitivity of Niraparib on A2780 cells Mol Cancer Ther. 2025 Mar 4;24(3):453-463.

Niraparib/尼拉帕尼 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice ID8 tumor model Oral 50 mg/kg Once daily for 3 weeks To evaluate the anti-tumor effect of Niraparib in the ID8 tumor model, results showed that Niraparib significantly inhibited tumor growth. Redox Biol. 2025 Mar;80:103528.
C57BL/6 mice ID8 ovarian cancer model Oral 40 mg/kg 5 days a week for 4 weeks To evaluate the effect of Niraparib on tumor growth, results showed that Niraparib significantly inhibited tumor growth. J Immunother Cancer. 2024 Oct 4;12(10):e009032
C57BL/6j mice Ovarian in situ tumor model Intramuscular injection and oral 50 mg/kg 3 times per week for 4 weeks The combination of P4 and Niraparib significantly prolonged the survival time of mice and reduced tumor volume. Research (Wash D C). 2024 May 24;7:0371
Mice RB1-KO xenograft mouse model Intraperitoneal injection 10 mg/kg Every 2 days for 30 days Niraparib treatment significantly reduced tumor volume and weight in RB1-KO mice, indicating that RB1 mutation enhances the antitumor efficacy of PARP inhibitors. JCI Insight. 2023 Nov 8;8(21):e165268.
C57BL/6 mice Ovarian cancer model Oral 25 mg/kg Four times a week for 52 days To investigate the effect of Niraparib on PD-L1 expression and its synergistic effect with PD-L1 blockade, results showed that Niraparib upregulated PD-L1 expression and synergistically inhibited tumor growth with PD-L1 blockade. J Transl Med. 2021 Oct 7;19(1):415.
Mice NSCLC mouse model Oral 80 mg/kg Once daily for 5 days on and 2 days off per week Niraparib significantly reduced the growth of PARhigh tumors, and this effect was similar in T cell-depleted mice, indicating that the antitumor effect of niraparib is independent of T cells J Immunother Cancer. 2022 Jun;10(6):e004280.
Nude mice A2780 ovarian cancer xenograft model Oral 40 mg/kg Once daily for 15 days To evaluate the tumor growth inhibitory effect of Niraparib combined with berberine, the results showed that the combination significantly inhibited tumor growth. Cell Death Dis. 2017 Oct 5;8(10):e3070.
C57BL/6JGpt mice ID8 EOC model Oral 50 mg/kg Once a day for 21 days To evaluate the effect of Niraparib on tumor growth and survival in ID8 EOC model mice Mol Cancer Ther. 2025 Mar 4;24(3):453-463.
C57BL/6j mice Ovarian in situ tumorigenesis model Intramuscular injection and gavage P4 (5 mg/kg) and niraparib (50 mg/kg) 3 times per week for 4 weeks Combination therapy of P4 and niraparib significantly reduced tumor volume and prolonged survival time in mice Research (Wash D C). 2024 May 24;7:0371

Niraparib/尼拉帕尼 动物研究

Dose Rat[4]: 3 mg/kg (i.v.), 5 mg/kg (p.o.) Mice: 25 mg/kg, 50 mg/kg[2] (p.o.), 100 mg/kg[2] (p.o.)
Administration i.v., p.o.

Niraparib/尼拉帕尼 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03705156 Platinum-sensitive Relapsed Ov... 展开 >>arian Cancer 收起 << Phase 3 Recruiting June 8, 2020 -
NCT03709316 Ovarian Cancer Phase 3 Recruiting June 30, 2021 -
NCT03574779 Ovarian Cancer Phase 2 Recruiting June 2020 United States, Massachusetts ... 展开 >> Dana-Farber Cancer Institute Recruiting Boston, Massachusetts, United States, 02215 United States, Oklahoma Stephenson Cancer Center Recruiting Oklahoma City, Oklahoma, United States, 73104 收起 <<

Niraparib/尼拉帕尼 参考文献

[1]Jones P, Altamura S, 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]Wang L, Mason KA, et al. MK-4827, a PARP-1/-2 inhibitor, strongly enhances response of human lung and breast cancer xenografts to radiation. Invest New Drugs. 2012 Dec;30(6):2113-20.

[3]Javle M, Curtin NJ, et al. The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy. Ther Adv Med Oncol. 2011 Nov;3(6):257-67.

Niraparib/尼拉帕尼 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.21mL

6.24mL

3.12mL

Niraparib/尼拉帕尼 技术信息

CAS号1038915-60-4
分子式C19H20N4O
分子量 320.39
SMILES Code O=C(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12)N
MDL No. MFCD17779309
别名 MK-4827( 尼拉帕尼) ;MK-4827
运输蓝冰
InChI Key PCHKPVIQAHNQLW-CQSZACIVSA-N
Pubchem ID 24958200
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, 2-8°C
溶解方案

DMSO: 25 mg/mL(78.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

Tags: Niraparib | MK-4827 | MK-4827( 尼拉帕尼) | PARP | AmBeed-信号通路专用抑制剂 | Niraparib/尼拉帕尼 纯度/质量文件 | Niraparib/尼拉帕尼 亚型比较 | Niraparib/尼拉帕尼 生物活性 | Niraparib/尼拉帕尼 动物研究 | Niraparib/尼拉帕尼 临床数据 | Niraparib/尼拉帕尼 参考文献 | Niraparib/尼拉帕尼 实验方案 | Niraparib/尼拉帕尼 技术信息

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