532912 CIP2A Inhibitor, TD-19 - Calbiochem

532912
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₃₀H₂₄N₄O₃

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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
      Quality LevelMQ100
      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.