Name | 7-chloro-5-(1H-pyrrol-2-yl)-1,3-dihydro-1,4-benzodiazepin-2-one |
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Synonyms |
2H-1,4-Benzodiazepin-2-one,7-chloro-1,3-dihydro-5-pyrrol-2-yl
UNII-DLH4T68L7I Ro 5-3335 |
Description | 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[1]. |
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Related Catalog | |
Target |
RUNX1-CBFβ interaction[1] |
In Vitro | 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[1]. Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos[1]. 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[1]. |
In Vivo | Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models[1]. Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish[1]. Ro5-3335 (300 mg/kg/d; p.o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model[1]. Animal Model: C57BL/6 mice (leukemic model)[1] 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. |
References |
Density | 1.46g/cm3 |
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Boiling Point | 501.6ºC at 760mmHg |
Melting Point | 256 °C (分解) |
Molecular Formula | C13H10ClN3O |
Molecular Weight | 259.69100 |
Flash Point | 257.1ºC |
Exact Mass | 259.05100 |
PSA | 57.25000 |
LogP | 2.03120 |
Index of Refraction | 1.712 |
Storage condition | 2-8℃ |
Hazard Codes | Xi |
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