532912 CIP2A Inhibitor, TD-19 - Calbiochem

532912
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₃₀H₂₄N₄O₃

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.32912.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number532912
          Brand Family Calbiochem®
          SynonymsN4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19
          DescriptionCIP2A Inhibitor, TD-19
          References
          ReferencesChao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.
          Product Information
          FormOff-white solid
          Hill FormulaC₃₀H₂₄N₄O₃
          Chemical formulaC₃₀H₂₄N₄O₃
          Applications
          Biological Information
          Primary TargetCIP2A
          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 -20°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

          CIP2A Inhibitor, TD-19 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Chao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.
          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.

          Revision09-September-2016 JSW
          SynonymsN4-(3-ethynylphenyl)-6,7-dimethoxy-N2-(4-phenoxyphenyl)quinazoline-2,4-diamine, TD19
          DescriptionA cell-permeable chemically modified derivative of erlotinib that is shown to be more effective in inducing apoptosis in H358, H441, H460, and A549 lung cancer cell lines (~10 µM). Highly effective in reducing the viability and inducing apotosis in erlotinib resistantH460 cells over-expressing CIP2A (cancerous inhibitor of protein phosphatase 2A ) that are resistant to erlotinib. Exhibits low binding affinity to the ATP binding site of the EGFR tyrosine kinase domain and has minimal effect on the phosphorylation of EGFR. Its anti-tumor effects are shown to be mediated via down-regulation of CIP2A and p-AKT expression and increased PP2A activity. Suppresses the growth of H460 xenograft tumors in NCr nude mice by approximately 80% (10 mg/kg. p.o. daily).
          FormOff-white solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₃₀H₂₄N₄O₃
          Purity≥98% by HPLC
          SolubilityDMSO (10 mg/ml with warming; solution will fall out of solution at room temperature) or DMF
          Storage -20°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
          ReferencesChao, T.T., et al. 2014. J. Pharm. Exp. Ther. 351,352.