产品
编 号:F762976
分子式:C62H76Cl2F2N14O11S2
分子量:1366.39
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生物活性:
GXH-II-052 is a potent bivalent bromodomain and extraterminal domain (BET) inhibitor. GXH-II-052 shows binding potential for BRD4-1, BRD4-2, BRD4-T, BRDT-1, BRDT-2, BRDT-T with Kd values of 28, 9.1, 4.8, 0.6, 8.4, 2.6 nM, respectively. GXH-II-052 shows antiproliferative activity. GXH-II-052 decreases the expression of c-Myc.

体内研究:
GXH-II-052 shows metabolic stability in mouse and human liver microsomes with an T1/2 values of 33, 3.6 min, respectively.

体外研究:
GXH-II-052 (0-10 μM; 72 h) shows antiproliferative activity with an IC50 value of 59 nM in MM1.S cells.GXH-II-052 (0-10 μM; 6 h) decreases the expression of c-Myc in a dose dependent manner.
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