Niraparib tosylate hydrate

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Chemical Structure| 1613220-15-7 同义名 : MK-4827 tosylate hydrate
CAS号 : 1613220-15-7
货号 : A1006359
分子式 : C26H30N4O5S
纯度 : 98%
分子量 : 510.61
MDL号 : MFCD28167748
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

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
动物实验配方：
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].
实验方案
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
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.