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Alobresib
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。
Alobresib图片
CAS NO:1637771-14-2
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Alobresib (GS-5829) 是一种 BET 溴结构域抑制剂,Alobresib 可用于治疗复发且耐药的过表达 c-Myc 的子宫浆液性癌。
Cas No.1637771-14-2
别名GS-5829
Canonical SMILESOC(C1=CC=CC=N1)(C2=CC=CC=N2)C3=C(NC(C4CC4)=N5)C5=CC(C(C(C)=NO6)=C6C)=C3
分子式C26H23N5O2
分子量437.49
溶解度DMSO: 83.33 mg/mL (190.47 mM)
储存条件Store at -20°C
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

Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc[1]. BET bromodomain[1]

Alobresib (0.1 nM-100 μM; 72 hours) inhibits cell proliferation in primary uterine serous carcinoma (USC) lines[1]. Cell Proliferation Assay[1] Cell Line: Primary uterine serous carcinoma (USC) lines ARK1 and ARK2 cell lines

Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) impaires USC-ARK2 xenograft tumor growth in female CB17/lcrHsd-Prkd/scid mice. Alobresib exhibits a significantly slower rate of tumor growth in mice, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.)[1]. Alobresib (10 and 20 mg/kg; oral; twice-daily; for 28 days) is well tolerated with no clear impact on body weight compared with vehicle control[1]. Animal Model: Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors[1]

[1]. Bonazzoli E, et al. Inhibition of BET Bromodomain Proteins with GS-5829 and GS-626510 in Uterine Serous Carcinoma, a Biologically Aggressive Variant of Endometrial Cancer. Clin Cancer Res. 2018 Oct 1;24(19):4845-4853.