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

219506
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      Overview

      Replacement Information

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      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      219506-10MG
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          Glass bottle 10 mg
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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
          Applications
          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

          Documentation

          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 +2°C to +8°C
          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.
          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.