性能参数

产品名称

MK-4827 hydrochloride

规格

5mg 10mg 50mg 100mg

货号

GOY-Y3319

 含量

>99.00%

CAS

1038915-64-8

别名

N/A

化学名

2-[4-[(3S)-piperidin-3-yl]phenyl]indazole-7-carboxamide;hydrochloride

分子式

C19H21ClN4O

分子量

分子量 356.85

溶解度

Soluble in DMSO

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

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

Niraparib inhibits PARP activity with EC50=4 nM and EC90=45 nM in a whole cell assay. Niraparib inhibits proliferation of cancer cells with mutant BRCA-1 and BRCA-2 with CC50 in the 10?100 nM range. Niraparib 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 inhibits PARP in these cell lines, A549 and H1299 cells are treated with 1 μM Niraparib for various times and measured PARP enzymatic activity using a chemiluminescent assay. The results show that Niraparib 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].

Niraparib is well tolerated and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib is well tolerated in vivo and demonstrates efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer. Niraparib 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 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].

1,2,3—**氧基苯  634-36-6  6-庚炔醇  63478-76-2

2-甲氧基-5-甲磺?；郊姿峒柞? 63484-12-8  2,4,6-三氯苯胺  634-93-5

3-氯苯硼酸  63503-60-6  苯基丁二酸  635-51-8

2-甲基-6-喹啉羧酸  635-80-3  4-氯-2,5-二甲氧基苯胺  6358-64-1

5-氯代水杨醛  635-93-8  2,5-二氯苯甲醛  6361-23-5

乙酸银  63-63-3  Boc-D-丝氨酸  6368-20-3

Unifiram25 mg 50 mg 100 mg 250 mg>98.00%Cas No. 272786-64-8C13H15FN2O3S

U913561mg 5mg 10mg 20mg>98.00%Cas No. 152886-85-6C13H17N3O

Wf-5161mg 5mg 10mg 20mg>98.00%Cas No. 310392-94-0C25H25Cl2N3O4

WAY-100635 maleate salt5mg 10mg 25mg 50mg>98.00%Cas No. 634908-75-1C29H38N4O6

VUF 1016610mg 50mg 500mg 1g>98.00%Cas No. 155584-74-0C13H15ClN4

VU04674855mg 10mg 50mg 100mg>98.00%Cas No. 1451994-10-7C17H17FN4O2S

VU0364572 (trifluoroacetate salt)1mg 5mg 10mg 25mg>98.00%Cas No. 1240514-89-9C21H31N3O3 ? CF3COOH