CB-5083

CB-5083CAS号: 1542705-92-9分子式: C24H23N5O2分子量: 413.4描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models .

纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
CB5083
外观
Powder
可溶性/溶解性
DMSO:83 mg/mL (200.74 mM)
生物活性
靶点
p97
In vitro(体外研究)
Treatment of tumor cells with CB-5083 leads to significant accumulation of markers associated with inhibition of ubiquitin−proteasome system and endoplasmic reticulum-associated degradation functions, which induces irresolvable proteotoxic stress and cell death
In vivo(体内研究)
In tumor bearing mice, oral administration of CB-5083 causes rapid accumulation of markers of the unfolded protein response and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. CB-5083 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors.

分子结构图

CB-5083