Ro5-3335

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.

Product information

CAS Number: 30195-30-3

Molecular Weight: 259.69

Formula: C13H10ClN3O

Chemical Name: 7-chloro-5-(1H-pyrrol-2-yl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one

Smiles: O=C1CN=C(C2=CC=CN2)C2=CC(Cl)=CC=C2N1

InChiKey: XWNMORIHKRROGW-UHFFFAOYSA-N

InChi: InChI=1S/C13H10ClN3O/c14-8-3-4-10-9(6-8)13(11-2-1-5-15-11)16-7-12(18)17-10/h1-6,15H,7H2,(H,17,18)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

In Vivo:

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.

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.

Products are for research use only. Not for human use.