产品
编 号:F311247
分子式:C13H10ClN3O
分子量:259.69
产品类型
结构图
CAS No: 30195-30-3
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生物活性:
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation.
体内研究:
Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models.?Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish.?Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model.Animal Model:C57BL/6 mice (leukemic model)
Dosage:300 mg/kg
Administration:Oral administration; daily; for 30 days
Result:Reduced the number of c-kit+ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen.
体外研究:
Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively.?Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos.?Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex.