475965 | c-Myc Inhibitor III, Mycro2 - Calbiochem

475965
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₁F₃N₄OS₂

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.