Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC50s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.
体外研究
Romidepsin (0-72 hours; 0-80 nM) inhibits proliferation of HCC cells in dose-dependent manner.
Romidepsin (0-48 hours; 0-60 nM) leads to a time- and dose-dependent induction of cell cycle arrest in the G2/M phase in HCC cells.
Romidepsin (0-48 hours; 0-60 nM) promotesapoptosis in HCC cells, increases c-caspase-3, c-caspase-9, and c-PARP protein expression.
Increaesd c-caspase-3, c-caspase-9, and c-PARP expression in HCC cells.
体内研究
Romidepsin (intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days) inhibited the tumor growth, reveals a higher expression of p-cdc25C, ki67, c-caspase-3 and c-PARP, and a lower expression of Ki-67 in Romidepsin treated tumors .
Animal Model:
Nude mice with Huh7 cells
Dosage:
0.5 and 1 mg/kg
Administration:
Intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days
Result:
Suppressed tumor growth in mouse xenograft models.
分子式
C24H36N4O6S2
分子量
540.70
CAS号
128517-07-7
中文名称
罗米地辛
运输条件
Room temperature in continental US; may vary elsewhere.