100082 | 14-3-3 Antagonist II, BV02 - Calbiochem

100082
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      Overview

      Key Spec Table

      Empirical Formula
      C₂₀H₁₇N₃O₆

      Pricing & Availability

      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      100082-10MG
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      Discontinued
      There is a newer version of this product
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          10 mg
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          Description
          Overview A cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation.
          Catalogue Number 100082
          Brand Family Calbiochem®
          Synonyms 2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
          References
          References Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.
          Product Information
          Form Off-white powder
          Hill Formula C₂₀H₁₇N₃O₆
          Chemical formula C₂₀H₁₇N₃O₆
          Molar Mass 395.4
          Structure formula Image
          Applications
          Biological Information
          Purity ≥98% by HPLC
          Physicochemical Information
          Solubility DMSO
          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 Regulatory Review
          Storage +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze No
          Special Instructions Following 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

          MSDS

          Languages
          English

          Certificates of Analysis

          TitleLot Number
          100082

          References

          Reference overview
          Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.

          Brochure

          Title
          Materials for Li-ion batteries and double-layer capacitors
          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.

          Revision 02-April-2012 JSW
          Synonyms 2-(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-ylcarbamoyl)terephthalic acid
          Description A cell-permeable, non-peptidyl pyrazolylcarbamoyl compound that targets the amphipathic client protein-binding groove of 14-3-3 and effectively competes against cellular pro-apoptotic c-Abl and cell cycle inhibitor protein p27Kip1 (CDK inhibitor 1B) for 14-3-3ς interaction, leading to c-Abl mitochondrial membrane relocation, c-Abl and p27Kip1 nuclear translocation, sub-G1 arrest, enhanced c-Abl cleavage, caspase-9 and -8 activation (24 h 5 µM treatment), and eventual apoptotic cell death in pro-B murine Ba/F3 lines expressing wt, E255K, or T315I Bcr-Abl (LD50 = 0.41, 1.30, 1.47 µM, respectively;). Also demonstrated to exhibit antiproliferative activity against the survival of three primary IM- (Imatinib mesylate; STI571) resistant CD34+ cultures (LD50 = 0.5, 0.7, and 2.5 µM) from CML (chronic myeloid leukemia) patients with T315I Bcr-Abl mutation.
          Form Off-white powder
          Intert gas (Yes/No) Packaged under inert gas
          Molar mass 395.4
          Chemical formula C₂₀H₁₇N₃O₆
          Structure formula
          Purity ≥98% by HPLC
          Solubility DMSO (5 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          No
          Special Instructions Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Regulatory Review
          References Mancini, M., et al. 2011. J. Pharmacol. Exp. Ther. 336, 596.