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.
IC50&Target
RUNX1-CBFβ interaction
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.
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.
分子式
C13H10ClN3O
分子量
259.69
CAS号
30195-30-3
运输条件
Room temperature in continental US; may vary elsewhere.