Niraparib (Synonyms: 尼拉帕尼; MK-4827)

目录号: HY-10619 纯度: 99.96%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Niraparib Chemical Structure

CAS No. : 1038915-60-4

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥682	In-stock
5 mg	￥620	In-stock
10 mg	￥1050	In-stock
50 mg	￥1900	In-stock
100 mg	￥3100	In-stock
500 mg	现货	询价
1 g		询价
5 g		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Niraparib:

MCE 顾客使用本产品发表的 57 篇科研文献

Proliferation Assay

: Niraparib purchased from MCE. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568. [Abstract]; CDK4 is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.

: Niraparib purchased from MCE. Usage Cited in: Appl Microbiol Biotechnol. 2019 Dec;103(23-24):9557-9568. [Abstract]; Cyclin D is evaluated via western blot analysis in different cell lines with the treatment of Niraparib in different concentrations and times.

: Niraparib purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2017 Oct;80(4):861-867. [Abstract]; PARP1 inhibition is lethal to MPM cells. Colony formation assays of clonal cell survival with continuous Niraparib or AZD2281.

Niraparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

查看所有亚型

PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

生物活性
纯度 & 产品资料
参考文献

生物活性

Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC₅₀s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity^[1]^[2]^[3].

IC₅₀ & Target^[1]

PARP-2

2.1 nM (IC₅₀)

PARP-1

3.8 nM (IC₅₀)

V-PARP

330 nM (IC₅₀)

TANK-1

570 nM (IC₅₀)

PARP-3

1300 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A2780	IC₅₀	4 nM Compound: 8, MK-4827	Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in human A2780 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
A549	CC₅₀	11 nM Compound: 8, MK-4827	Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human A549 cells transfected with BRCA2 shRNA assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
A549	CC₅₀	1760 nM Compound: 8, MK-4827	Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against wild type human A549 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
BT-20	CC₅₀	2200 nM Compound: 8, MK-4827	Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human BT20 cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
CAPAN-1	IC₅₀	3.5 nM Compound: 8, MK-4827	Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in BRCA2-deficient human CAPAN-1 cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
CAPAN-1	CC₅₀	90 nM Compound: 56, MK-4827	Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay Antiproliferative activity against human Capan1 cells expressing BRCA2 6174delT mutation and loss of wild-type allele after 13 days by cell titer-blue assay	[PMID: 19873981]
DLD-1	IC₅₀	0.149 μM Compound: 3	Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days Antiproliferative activity against human DLD-1 deficient in BRCA-2 cells measured after 7 days	[PMID: 34570508]
DoTc2-4510	CC₅₀	23 nM Compound: 8, MK-4827	Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human DoTc2-4510 cells carrying BRCA2 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HeLa	CC₅₀	33 nM Compound: 56, MK-4827	Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay	[PMID: 19873981]
HeLa	CC₅₀	34 nM Compound: 8, MK-4827	Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HeLa	EC₅₀	4 nM Compound: 8, MK-4827	Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay	[PMID: 25761096]
HeLa	CC₅₀	852 nM Compound: 8, MK-4827	Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against wild type human HeLa cells assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]
HeLa	CC₅₀	860 nM Compound: 56, MK-4827	Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay	[PMID: 19873981]
HMEC	CC₅₀	> 5000 nM Compound: 56, MK-4827	Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay Antiproliferative activity against HMEC after 6 to 7 days by cell titer-blue assay	[PMID: 19873981]
HT-22	IC₅₀	35 μM Compound: 50	Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay Cytotoxicity against mouse HT-22 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay	[PMID: 36876904]
Jurkat	EC₅₀	0.2 μM Compound: MK-4827	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay in presence of 100 uM of temozolomide	[PMID: 23850199]
Jurkat	EC₅₀	31 μM Compound: MK-4827	Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay Inhibition of PARP1 in human Jurkat cells assessed as reduction of cell viability after 96 hrs by MTS assay	[PMID: 23850199]
MDA-MB-231	IC₅₀	33.22 μM Compound: Niraparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs by CCK-8 assay	[PMID: 36512711]
MDA-MB-231	IC₅₀	60.91 μM Compound: Niraparib	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs in presence of nutlin-3 by CCK-8 assay	[PMID: 36512711]
MDA-MB-436	CC₅₀	18 nM Compound: 56, MK-4827	Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay Antiproliferative activity against human MDA-MB-436 cells expressing BRCA1 5396 + 1G>A mutant after 6 days by cell titer-blue assay	[PMID: 19873981]
MDA-MB-468	IC₅₀	7.6 μM Compound: Niraparib	Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay Cytotoxicity against human MDA-MB-468 cells measured after 72 hrs by Celltiter-Glo assay	[PMID: 33200929]
PrEC	CC₅₀	> 5000 nM Compound: 56, MK-4827	Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay Antiproliferative activity against human PrEC cells after 6 to 7 days by cell titer-blue assay	[PMID: 19873981]
SUM149PT	CC₅₀	24 nM Compound: 8, MK-4827	Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay Cytotoxicity against human SUM149PT cells carrying BRCA1 mutant assessed as inhibition of cell proliferation after 5 to 7 days by CellTiter-Blue assay	[PMID: 25761096]

体外研究
(In Vitro)

Niraparib (MK-4827) 在全细胞测定中抑制 PARP 活性，EC₅₀=4 nM，EC₉₀=45 nM。Niraparib 抑制突变型 BRCA-1 和 BRCA-2 癌细胞的增殖，CC₅₀ 在 10-100 nM 范围内。Niraparib 在全细胞测定中分别表现出优异的 PARP 1 和 2 抑制效果^[1]。为了验证 Niraparib (MK-4827) 在这些细胞系中抑制 PARP，用 1 μM Niraparib 处理 A549 和 H1299 细胞不同时间，并使用化学发光测定法测量 PARP 酶活性。结果表明，Niraparib 在治疗后 15 分钟内抑制 PARP，在 A549 细胞中 1 小时的抑制率达到约 85%，在 H1299 细胞中 1 小时的抑制率达到约 55%^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Niraparib 在体内耐受性良好，在 BRCA-1 缺陷癌症异种移植模型中作为单一药物表现出疗效。Niraparib (MK-4827) 的特点是大鼠的药代动力学可接受，血浆清除率为 28 (mL/min)/kg，分布容积极高 (Vd_ss=6.9 L/kg)，终末半衰期长 (t_1/2=3.4 h)，生物利用度极高，F=65%^[1]。Niraparib 在两种情况下均增强了 p53 突变型 Calu-6 肿瘤的放射反应，单日剂量 50 mg/kg 比每日两次 25 mg/kg 更有效^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female nude mice (Ncr Nu/Nu) with solitary tumor xenografts^[3]
Dosage:	25 mg/kg or 50 mg/kg
Administration:	Gavage, 25 mg/kg twice a day with 6 h between doses or 50 mg/kg once daily for 21 consecutive days
Result:	Enhanced radiation response.

Clinical Trial

分子量

320.39

Formula

C₁₉H₂₀N₄O

CAS 号

1038915-60-4

性状

固体

颜色

White to light yellow

中文名称

尼拉帕尼

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
In solvent	-80°C	1 year
	-20°C	6 months

溶解性数据

细胞实验：

DMSO 中的溶解度 : 31.25 mg/mL (97.54 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1212 mL	15.6060 mL	31.2120 mL
5 mM	0.6242 mL	3.1212 mL	6.2424 mL
10 mM	0.3121 mL	1.5606 mL	3.1212 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.49 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.49 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
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 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.49 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.96%

选择批次：

Data Sheet (649 KB) SDS (393 KB)

COA (285 KB) HNMR (272 KB) LCMS (237 KB)

产品使用指南 (1538 KB)

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. [Content Brief]

[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. [Content Brief]

[3]. Wang L, 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. [Content Brief]

[4]. Mirza MR, et al. Niraparib Maintenance Therapy in Platinum-Sensitive, Recurrent Ovarian Cancer. N Engl J Med. 2016 Dec 1;375(22):2154-2164. [Content Brief]

Niraparib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.1212 mL	15.6060 mL	31.2120 mL	78.0299 mL
	5 mM	0.6242 mL	3.1212 mL	6.2424 mL	15.6060 mL
	10 mM	0.3121 mL	1.5606 mL	3.1212 mL	7.8030 mL
	15 mM	0.2081 mL	1.0404 mL	2.0808 mL	5.2020 mL
	20 mM	0.1561 mL	0.7803 mL	1.5606 mL	3.9015 mL
	25 mM	0.1248 mL	0.6242 mL	1.2485 mL	3.1212 mL
	30 mM	0.1040 mL	0.5202 mL	1.0404 mL	2.6010 mL
	40 mM	0.0780 mL	0.3901 mL	0.7803 mL	1.9507 mL
	50 mM	0.0624 mL	0.3121 mL	0.6242 mL	1.5606 mL
	60 mM	0.0520 mL	0.2601 mL	0.5202 mL	1.3005 mL
	80 mM	0.0390 mL	0.1951 mL	0.3901 mL	0.9754 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

Niraparib (Synonyms: 尼拉帕尼; MK-4827)

Customer Review

Other Forms of Niraparib:

MCE 顾客使用本产品发表的 57 篇科研文献

Niraparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Niraparib 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

Niraparib (Synonyms: 尼拉帕尼; MK-4827)

Customer Review

Other Forms of Niraparib:

Niraparib 相关抗体

MCE 顾客使用本产品发表的 57 篇科研文献

Niraparib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 PARP 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Niraparib 相关抗体:

摩尔计算器

稀释计算器

Niraparib 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z