30195-30-3
30195-30-3 結(jié)構(gòu)式
基本信息
NSC-66020
CBFβ-Runx1 inhibitor II
CBFβ-Runx1 inhibitor II
7-Chloro-5-(1H-pyrrol-2-yl)-1H-benzo[e][1,4]diazepin-2(3H)-one
7-Chloro-5-(1H-pyrrol-2-yl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one
7-Chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-2H-1,4-benzodiazepin-2-one
7-Chloro-2-oxo-5-(1H-pyrrol-2-yl)-2,3-dihydro-1H-1,4-benzodiazepine
2H-1,4-Benzodiazepin-2-one, 7-chloro-1,3-dihydro-5-(1H-pyrrol-2-yl)-
Ro5-3335,Ro53335,CBFβ,inhibit,binding,Ro-5-3335,core,RUNX1,RUNX1-CBFB,factor,CBF,interaction,leukemia,Inhibitor,Ro5 3335
常見(jiàn)問(wèn)題列表
RUNX1-CBFβ interaction
Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC
50
s 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.
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. |