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

219506
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Número de referenciaEmbalaje Cant./Env.
219506-10MG Frasco de vidrio 10 mg
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

CBFβ-Runx1 Inhibitor II, Ro5-3335 - CAS 30195-30-3 - Calbiochem Certificados de análisis

CargoNúmero de lote
219506

Referencias bibliográficas

Visión general referencias
Cunningham, L, et al. 2012. Proc Natl Acad Sci USA. 109, 14594.
Witvrouw, M., et al. 1992. Antimicrob Agents Chemother. 36, 2628.
Ficha técnica

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.