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.
A progressive, dose response decrease in cell proliferation. IC50s of 27 nM and 31 nM for ARK2 and ARK1 cells, respectively.
体内研究
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.).
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.
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.).
分子式
C26H23N5O2
分子量
437.49
CAS号
1637771-14-2
运输条件
Room temperature in continental US; may vary elsewhere.