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Niraparib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Niraparib图片
CAS NO:1038915-60-4

尼拉帕尼
MK-4827
Niraparib (MK-4827) 是高效的,具有生物口服利用度的PARP1PARP2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 bioavailablePARP1andPARP2inhibitor withIC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activatesapoptosisand 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)

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 CC50in 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[1]. 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[2].

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 (Vdss=6.9 L/kg), long terminal half-life (t1/2=3.4 h), and excellent bioavailability, F=65%[1]. 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[3].

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

性状

Solid

Formula

C19H20N4O

CAS 号

1038915-60-4

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(78.03 mM;Need ultrasonic)

H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 80℃)(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.1212 mL15.6060 mL31.2120 mL
5 mM0.6242 mL3.1212 mL6.2424 mL
10 mM0.3121 mL1.5606 mL3.1212 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.49 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.49 mM,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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (6.49 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在本网站选购。
 
 
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