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JNJ-64619178
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-64619178图片
CAS NO:2086772-26-9
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
1mg电议
5mg电议
10mg电议
50mg电议

产品介绍
JNJ-64619178 (Onametostat) 是一种选择性、口服活性和假不可逆的蛋白质精氨酸甲基转移酶 5 (PRMT5) 抑制剂,IC50 为 0.14 nM。 JNJ-64619178 在肺癌中具有有效的活性。
Cas No.2086772-26-9
别名Onametostat
化学名(1S,2R,3S,5R)-3-(2-(2-amino-3-bromoquinolin-7-yl)ethyl)-5-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol
Canonical SMILESBrC1=C(N)N=C(C=C(CC[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C(N=CN=C4N)=C4C=C3)C2)C=C5)C5=C1
分子式C22H23BrN6O2
分子量483.36
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (PRMT5-MEP-50, IC50=0.14 nM), good pharmacokinetic properties and safety.

JNJ-64619178 can be combined with a SAM binding pocket to inhibit the function of PRMT/MEP50 in a time-dependent manner.Various cell lines exhibited different degrees of sensitivity to JNJ-64619178, indicating that JNJ-64619178 inhibits PRMT5 mainly by genomic rather than general targeted cytotoxicity [1].

The methylation of SMD1/3 protein can be selectively and effectively prevented by oral administration of 10 mg/kg JNJ-64619178 per day.SMD1/3 is a key component of the splice and a substrate for PRMT5/MEP50.In the biomarker-driven human small cell lung cancer xenograft model (NCI-H1048), JNJ-64619178 can cause tumor regression and prolong tumor growth inhibition after termination of administration [1].

Reference:

[1] Dirk Brehmer, et al. 108th Annu Meet Am Assoc Cancer Research