Alobresib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Alobresib 是 BET 溴结构域抑制剂，是一种抗肿瘤候选化合物。

Alobresib is an inhibitor of BET bromodomain,is an antineoplastic drug candidate.in vitro experiments demonstrated high sensitivity of USC cell lines to the exposure to GS-5829, GS-626510, and JQ1 with BET inhibitors causing a dose-dependent decrease in the phosphorylated levels of c-Myc and a dose-dependent increase in caspase activation (apoptosis).?In comparative in vivo experiments, GS-5829 and/or GS-626510 were found more effective than JQ1 at the concentrations/doses used in decreasing tumor growth in both USC-ARK1 and USC-ARK2 mouse xenograft models.

Cell Proliferation Assay Cell Line:Primary uterine serous carcinoma (USC) lines ARK1 and ARK2 cell lines Concentration:0.1 nM, 10 nM, 1 μM, 100 μM Incubation Time:72 hours Result:A progressive, dose response decrease in cell proliferation. IC50s of 27 nM and 31 nM for ARK2 and ARK1 cells, respectively.

Animal Model:Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumorsDosage:10 and 20 mg/kg Administration:Oral; twice-daily; 28 days Result:Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

Vorolanib,GS-5829

Chromatin/Epigenetic

Epigenetic Reader Domain

BET

Cancer

Breast Cancer

1637771-14-2

437.5

C26H23N5O2

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (190.47 mM)

Cc1noc(C)c1-c1cc(c2nc([nH]c2c1)C1CC1)C(O)(c1ccccn1)c1ccccn1

——

(-20℃)

With Ice Pack

≥ 2 years