Alobresib

Research use only, not for human use.

Alobresib is an inhibitor of BET bromodomain,is an antineoplastic drug candidate.

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