产品
编 号:F399840
分子式:C18H13ClN2O3S
分子量:372.83
产品类型
结构图
CAS No: 593273-05-3
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产品详情
生物活性:
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity.
体内研究:
DCH36_06 (25-50 mg/kg; intraperitoneal injection; every two days; for 20 days) blocks the leukemic xenograft growth in mice.Animal Model:MV4-11 xenograft nude mice
Dosage:25 mg/kg, 50 mg/kg
Administration:Intraperitoneal injection; every two days; for 20 days
Result:The tumor growth rate showed significant reduction in dose-dependent manner.
体外研究:
DCH36_06 (6.7-20 μM; 24-48 hours) treatment arrests cell cycle at G1 phase and induces apotosis in a dose-dependent manner in leukemic cells.DCH36_06 (5-10 μM; 24 hours) treatment significantly activates the cleavage of pro-caspase 3, pro-caspase 9 and PARP1 at dose-dependent manner.DCH36_06 shows potent antiproliferative activity against tested leukemia cell lines (CEM, MOLT3, MOLT4, Jurkat, MV4-11, THP-1, RS4; 11, KOPN8, Kasumi-1 and K562 cells) in a dose-dependent manner with IC50 values at single-digit micromolar range.