219506

CBFβ-Runx1 Inhibitor II

• Synonym(s): CBFβ-Runx1 Inhibitor II, RUNX1/CBFβ inhibitor
• Linear Formula: C13H10ClN3O
• CAS Number: 30195-30-3
• UNSPSC Code: 12352200
• NACRES: NA.28

Properties

• form: (Off-white solid)
• Quality Level: 100
• storage condition: OK to freeze
• solubility: soluble (DMSO (50 mg/ml))
• storage temp.: 2-8°C

Description

General description

A cell-permeable benzodiazepine that suppresses CBFα/Runx1-CBFβ transactivation activity (by 42% in 293-0 cell-based reporter assay; [Ro5-3335] = 25 µM) via direct affinity bindings to both subunits of the heterodimeric transcription factor complex. Shown to inhibit oncogenic fusion CBFB-MYH11-, TEL-RUNX1-, and RUNX1-ETO-, dependent leukemia cells proliferation (IC50 = 1.1, 17.3, and 21.7 µM, respectively, in ME-1, REH, and Kasumi-1 cultures) in vitro and more effectively reduce peripheral blood c-kit+ population (300 mg/kg/d via animal feed on days 10 to 40 after transplant) than Cytarabine (Cat. No. 251010; 100 mg/kg/d via i.p. on days 10 to 14 after transplant) in a murine Cbfb-MYH11 leukemia transplant model (49%, 17.5%, and <1% c-kit+ cells, respectively, 21 days after transplant in saline, Cytarabine, and Ro5-3335 treatment group) in vivo. Comparing to CBFβ-Runx1 Inhibitor I (Cat. No. 219505), Ro5-3335 modulates the Runx1-CBFβ heterodimer formation without completely disrupting the subunits interaction.

Application

The CBFΒ-Runx1 Inhibitor II, Ro5-3335, also referenced under CAS 30195-30-3, suppresses CBFΑ/Runx1-CBFΒ transactivation activity (25 µM; 293-0 cells) via direct bindings to both subunits of the heterodimeric transcription factor complex.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable