475965 c-Myc Inhibitor III, Mycro2 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₁F₃N₄OS₂

Pricing & Availability

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475965-10MG
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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable pyrazolopyrimidine-carboxamide that selectively inhibits c-Myc-Max dimer DNA binding activity (IC50 = 23 µM) by preventing c-Myc-Max heterodimer formation, while affecting Max, Jun, C/EBPα homodimers, or Jun-Fos heterodimer DNA binding only at much higher concentrations (IC50 = ≥54 µM). Shown to selectively inhibit c-Myc-Max-dependent transcription (by 77% against E-Box promoter-driven reporter transcription at 10 µM), cancer proliferation, and anchorage-independent colony formation (Effective conc. 10-20 µM).
      Catalogue Number475965
      Brand Family Calbiochem®
      Synonyms5-(Thiophen-2-yl)-N-(thiophen-2-ylmethyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxamide
      References
      ReferencesKiessling, A., et al. 2006. Chem. Biol. 13, 745.
      Product Information
      FormYellow solid
      Hill FormulaC₁₇H₁₁F₃N₄OS₂
      Chemical formulaC₁₇H₁₁F₃N₄OS₂
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetα-helical dimerization motifs of c-Myc/Max factors
      Primary Target IC<sub>50</sub>IC₅₀ = 23 and 54 µM for c-Myc/Max and Max/Max dimerization
      Secondary targetα-helical dimerization motifs of Max/Max factors
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      c-Myc Inhibitor III, Mycro2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      c-Myc Inhibitor III, Mycro2 - Calbiochem Certificates of Analysis

      TitleLot Number
      475965

      References

      Reference overview
      Kiessling, A., et al. 2006. Chem. Biol. 13, 745.
      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.

      Revision29-September-2012 JSW
      Synonyms5-(Thiophen-2-yl)-N-(thiophen-2-ylmethyl)-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine-2-carboxamide
      DescriptionA cell-permeable pyrazolopyrimidine-carboxamide that selectively inhibits c-Myc-Max dimer DNA binding activity (IC50 = 23 µM) by preventing c-Myc-Max heterodimer formation, while affecting Max, Jun, C/EBPα homodimers, or Jun-Fos heterodimer DNA binding only at much higher concentrations (IC50 = 54 µM for Max-Max dimer and IC50 > >54 µM for the rest). Shown to selectively inhibit c-Myc-Max-dependent transcription (by 77%, 31%, and 19%, respectively, against E-Box, AP-1, and SRE promoter-driven reporter transcription with 10 µM inhibitior), anchorage-independent colony formation (By 40% and 2%, respectively, against c-Myc or v-Src transformed Rat1a cells with 15 µM inhibitor) and proliferation (Effective conc. 10-20 µM in Raji, MCF-7, and U2OS cultures), but not c-Myc-independent proliferation of PC-12 cells (by <10% at 20 µM).
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₁₁F₃N₄OS₂
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (100 mg/ml; clear, yellow solution)
      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 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesKiessling, A., et al. 2006. Chem. Biol. 13, 745.