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LLY-283
本半岛bd体育手机客户端 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。
LLY-283图片
CAS NO: 2040291-27-6
包装与价格:
包装 价格(元)
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
LLY-283是一种有效的,选择性的,可口服的蛋白精氨酸甲基转移酶5(PRMT5)抑制剂,对PRMT5:MEP50复合物的作用很强,IC50和Kd值分别为22nM和6nM,具有抗肿瘤活性。
Cas No. 2040291-27-6
Canonical SMILES O[C@H]1[C@@H](O[C@@]([C@@H](C2=CC=CC=C2)O)([H])[C@H]1O)N3C4=NC=NC(N)=C4C=C3
分子式 C17H18N4O4
分子量 342.35
溶解度 DMSO: 250 mg/mL (730.25 mM)
储存条件 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
半岛bd体育手机客户端 描述

LLY-283 is a potent, selective and oral protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM and a Kd of 6 nM for PRMT5:MEP50 complex, and shows antitumor activity.

LLY-283 is a potent, oral and selective arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 22 nM in vitro and 25 nM in cells, as well as a Kd of 6 nM for PRMT5:MEP50 complex in vitro; LLY-283 inhibits the proliferation of A375 cell with an IC50 of 46 nM[1].

LLY-283 (20 mg/kg; p.o., QD (once a day)) causes a significant inhibition on tumor growth in mice bearing A375 cells after treatment for 28 days[1].

[1]. Zahid Q. Bonday, et al. LLY-283, a Potent and Selective Inhibitor of Arginine Methyltransferase 5, PRMT5, with Antitumor Activity. ACS Med. Chem. Lett., 2018, 9 (7), pp 612-617.

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