產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 100mg
CAS	1038915-73-9
別名	N/A
化學(xué)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	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
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

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].

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

2. 為了您的安全和健康，請(qǐng)穿好實(shí)驗(yàn)服并佩戴一次性手套和口罩操作。

原創(chuàng)作者：上海莼試生物技術(shù)有限公司

在線咨詢

留言注意事項(xiàng)：

1.遵守中華人民共和國(guó)有關(guān)法律、法規(guī)，尊重網(wǎng)上道德，承擔(dān)一切因您的行為而直接或間接引起的法律責(zé)任。

2.請(qǐng)您真實(shí)的反映產(chǎn)品的情況,不要捏造、誣蔑、造謠。如對(duì)產(chǎn)品有任何疑問,也可以留言咨詢。

3.未經(jīng)本站同意，任何人不得利用本留言簿發(fā)布個(gè)人或團(tuán)體的具有廣告性質(zhì)的信息或類似言論。

您感興趣的產(chǎn)品*
您的單位*
聯(lián)系人*
聯(lián)系電話*
詳細(xì)地址*
常用郵箱*
請(qǐng)輸入您對(duì)我們的意見或建議*
驗(yàn)證碼*