JNJ-64619178 - PRMT5 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJNJ-64619178Cat. No.: HY-101564CAS No.: 2086772-26-9分式: CHBrNO分量: 483.36作靶点: Histone Methyltransferase作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (258.61 mM; N

2、eed ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0689 mL 10.3443 mL 20.6885 mL5 mM 0.4138 mL 2.0689 mL 4.1377 mL10 mM 0.2069 mL 1.0344 mL 2.0689 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根

3、据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.30 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.30 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.

4、30 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 JNJ-64619178种伪不可逆的、服有效的、选择性 PRMT5 抑制剂，IC50 为 0.14 nM。JNJ-64619178 有治疗肺癌的潜 1 2。IC50 & Target IC50: 0.14 nM (PRMT5) 2体外研究 JNJ-64619178 binds simultaneously to the S-adenosylmethionine (SAM)- and protein subst

5、rate- bindingpockets of the PRMT5/MEP50 complex with a pseudo-irreversible mode-of-action. JNJ-64619178 showspotent and broad inhibition of cellular growth 1.体内研究 Oral administration of JNJ-64619178 results in efficient inhibition of dimethylation of SMD1/3 proteins,components of the splicing machin

6、ery and direct substrates of the methylosome, in several non-small celllung cancer and small cell lung cancer cancer mouse xenograft models 1.REFERENCES1. Tongfei Wu, et al. Abstract 4859: JNJ-64619178, a selective and pseudo-irreversible PRMT5 inhibitor with potent in vitro and in vivoactivity, demonstrated in several lung cancer models.2. Tao H, et al. Discovery of Novel PRMT5 Inhibitors by Virtual Screening and Biological Evaluations. Chem Pharm Bull (Tokyo).2019;67(4):382-388.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use onl