性能参数

产品名称

MK-4827 tosylate

规格

5mg 10mg 50mg 100mg

货号

GOY-Y2877

 含量

>98.00%

CAS

1038915-73-9

别名

N/A

化学名

(S)-2-(4-(piperidin-3-yl)phenyl)-2H-indazole-7-carbimidic acid compound with 4-methylbenzenesulfonic acid (1:1)

分子式

C26H28N4O4S

分子量

分子量 492.59

溶解度

DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml,Ethanol: 1 mg/ml

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 tosylate (MK-4827 tosylate) is an excellent PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively.

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 CC50 in 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 Niraparib (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].

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].

Amberlite® XAD16非离子型大孔树脂 20-60 mesh  4,’6-二脒基-2-苯基吲哚二盐酸盐 98%

Amberlite XAD7HP 离子交换树脂 Mesh 20-60  二氢罗丹明123 95%

粒径0.49 - 0.69 mm  D-虫荧光素游离酸 98%

粒径:0.500 - 0.750 mm  D-虫荧光素钠盐 98%

16-50 目  D-荧光素磷酸盐 lyophilized powder

Amberlite XAD-1180N 非离子型多孔树脂 粒径0.350 -?

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