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Niraparib tosylate hydrate {[allProObj[0].p_purity_real_show]}

货号:A1006359 同义名: MK-4827 tosylate hydrate

Niraparib tosylate hydrate(MK-4827)对甲苯磺酸盐水合物是一种高效且口服可用的PARP1PARP2抑制剂,IC50值分别为3.8和2.1 nM。它抑制DNA损伤修复,激活凋亡,并表现出抗肿瘤活性。

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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 tosylate hydrate 化学结构 CAS号:1613220-15-7
Niraparib tosylate hydrate 化学结构
CAS号:1613220-15-7
Niraparib tosylate hydrate 3D分子结构
CAS号:1613220-15-7
Niraparib tosylate hydrate 化学结构 CAS号:1613220-15-7
Niraparib tosylate hydrate 3D分子结构 CAS号:1613220-15-7
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Niraparib tosylate hydrate 纯度/质量文件 产品仅供科研

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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

98+%
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 tosylate hydrate 生物活性

描述 Niraparib tosylate hydrate is a potent oral bioactive PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.Niraparib tosylate hydrate inhibits DNA damage repair, activates apoptosis, and displays antitumour activity[1][2][3].Niraparib tosylate hydrate inhibits PARP activity with EC50 value of 4 nM and EC90 value of 45 nM in whole-cell assay. Niraparib tosylate hydrate inhibits the proliferation of mutant BRCA-1 and BRCA-2 cancer cells with CC50 values in the range of 10-100 nM. Niraparib tosylate hydrate inhibited PARP 1 and PARP 2 very well, with IC50s of 3.8 and 2.1 nM in whole-cell assays, respectively[1].Niraparib tosylate hydrate inhibited PARP within 15 minutes of treatment, exhibiting approximately 85% inhibition in A549 cells within 1 hour and 55% inhibition in H1299 cells within 1 hour[2].

Niraparib tosylate hydrate 动物研究

Animal study Niraparib tosylate hydrate has an acceptable pharmacokinetic profile in rats, with a plasma clearance of 28 (mL/min)/kg, a very large volume of distribution (Vdss=6.9 L/kg), a long terminal half-life (t1/2=3.4 h), and a high bioavailability (F=65%)[1].Niraparib tosylate hydrate potentiated the radiation response in p53 mutant Calu-6 tumours in both cases, with a single daily dose of 50 mg/kg being more effective than two daily doses of 25 mg/kg[3].

Niraparib tosylate hydrate 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.

[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.

Niraparib tosylate hydrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.79mL

1.96mL

0.98mL

19.58mL

3.92mL

1.96mL

Niraparib tosylate hydrate 技术信息

CAS号1613220-15-7
分子式C26H30N4O5S
分子量 510.61
SMILES Code O=C(C1=CC=CC2=CN(C3=CC=C([C@H]4CNCCC4)C=C3)N=C12)N.O=S(C5=CC=C(C)C=C5)(O)=O.[H]O[H]
MDL No. MFCD28167748
别名 MK-4827 tosylate hydrate
运输蓝冰
InChI Key ACNPUCQQZDAPJH-FMOMHUKBSA-N
Pubchem ID 74763937
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 50 mg/mL(97.92 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
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