30195-30-3

30195-30-3 structure

Name: Ro 5-3335
Chemical Name: 7-chloro-5-(1H-pyrrol-2-yl)-1,3-dihydro-1,4-benzodiazepin-2-one
CAS Number: 30195-30-3
Molecular Formula: C₁₃H₁₀ClN₃O
Molecular Weight: 259.69100
Catalog: Signaling Pathways Others Others
Create Date: 2016-11-21 18:17:16
Modify Date: 2024-01-08 15:53:51
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].

Name	7-chloro-5-(1H-pyrrol-2-yl)-1,3-dihydro-1,4-benzodiazepin-2-one
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].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
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	[1]. Cunningham L, et al. Identification of benzodiazepine Ro5-3335 as an inhibitor of CBF leukemia through quantitative high throughput screen against RUNX1-CBFβ interaction. Proc Natl Acad Sci U S A. 2012 Sep 4;109(36):14592-7.

Density	1.46g/cm3
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

1622-61-3	2011-67-8
40790-04-3	30195-30-3