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219506 CBFβ-Runx1 Inhibitor II, Ro5-3335 - CAS 30195-30-3 - Calbiochem

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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: [7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFα-CBFβ Inhibitor II

219506
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      Description
      OverviewA cell-permeable benzodiazepine that suppresses CBFα/Runx1-CBFβ transactivation activity (25 µM; 293-0 cells) via direct 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 to 21.7 µM) in vitro and more effectively reduce peripheral blood c-kit+ population (300 mg/kg/d via animal feed) than Cytarabine (Cat. No. 251010) in a murine Cbfb-MYH11 leukemia model 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.
      Catalogue Number219506
      Brand Family Calbiochem®
      Synonyms[7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFα-CBFβ Inhibitor II
      References
      ReferencesCunningham, L, et al. 2012. Proc Natl Acad Sci USA. 109, 14594.
      Witvrouw, M., et al. 1992. Antimicrob Agents Chemother. 36, 2628.
      Product Information
      CAS number30195-30-3
      FormOff-white solid
      Hill FormulaC₁₃H₁₀ClN₃O
      Chemical formulaC₁₃H₁₀ClN₃O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationThe 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.
      Biological Information
      Primary Target IC<sub>50</sub>0.5 µM
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      219506-10MG 04055977218084

      Documentation

      CBFβ-Runx1 Inhibitor II, Ro5-3335 - CAS 30195-30-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      219506

      References

      Reference overview
      Cunningham, L, et al. 2012. Proc Natl Acad Sci USA. 109, 14594.
      Witvrouw, M., et al. 1992. Antimicrob Agents Chemother. 36, 2628.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision11-April-2013 JSW
      Synonyms[7-chloro-5-(2-pyrryl)-3H-1,4 benzodiazapin-2-(H)-one], Ro53335, CBFα-CBFβ Inhibitor II
      DescriptionA 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.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number30195-30-3
      Chemical formulaC₁₃H₁₀ClN₃O
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesCunningham, L, et al. 2012. Proc Natl Acad Sci USA. 109, 14594.
      Witvrouw, M., et al. 1992. Antimicrob Agents Chemother. 36, 2628.