475857 | Mirk/Dyrk1B Inhibitor, Compound A - Calbiochem

475857
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₁₇Cl₂N₅O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475857-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable dihydropyridopyrimidine-carboxamide compound that acts as a potent and reversible inhibitor of Mirk/Dyrk1B and Dyrk1A kinases (IC50 = 68 and 22 nM). Exhibits very high selectivity for Mirk/Dyrk1B compared to Abl, Flt3, and MARK1 (64, 56 and 73% inhibition at 10 µM, respectively) and a panel of 46 other kinases. Shown to induce activation of caspase-3 and sensitize tumor cells to the action of gemcitabine and cisplatin (Cat. No. 232120), possibly by de-stabilizing p27. Preferentially increases cycling in Mirk-elevated quiescent pancreatic cancer cells (SU86.86, Panc1, AsPc1, and SW620 at ~1 µM). Also, shown to increase level of superoxides in quiescent pancreatic tumor cells (Panc1, SU86.86, and AsPc1) by blocking SOD2 and SOD3 activities.
          Catalogue Number475857
          Brand Family Calbiochem®
          SynonymsN-(2-Chloro-5-(3-chlorobenzylcarbamoyl)phenyl)-2-methoxy-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, N-(2-Chloro-5-((3-chlorobenzyl)carbamoyl)phenyl)-7-hydroxy-2-methoxypyrido[2,3-d]pyrimidine-6-carboxamide
          References
          ReferencesEwton, D.Z., et al. 2011. Mol. Cancer Ther. 10, 2104.
          Product Information
          FormWhite solid
          Hill FormulaC₂₃H₁₇Cl₂N₅O₄
          Chemical formulaC₂₃H₁₇Cl₂N₅O₄
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥99% 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 +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) 

          References

          Reference overview
          Ewton, D.Z., et al. 2011. Mol. Cancer Ther. 10, 2104.
          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.

          Revision22-February-2013 JSW
          SynonymsN-(2-Chloro-5-(3-chlorobenzylcarbamoyl)phenyl)-2-methoxy-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, N-(2-Chloro-5-((3-chlorobenzyl)carbamoyl)phenyl)-7-hydroxy-2-methoxypyrido[2,3-d]pyrimidine-6-carboxamide
          DescriptionA cell-permeable dihydropyridopyrimidine-carboxamide compound that acts as a potent and reversible inhibitor of Mirk/Dyrk1B and Dyrk1A kinases (IC50 = 68 and 22 nM). Exhibits very high selectivity for Mirk/Dyrk1B compared to Abl, Flt3, and MARK1 (64, 56 and 73% inhibition at 10 µM, respectively) and a panel of 46 other kinases. Shown to induce activation of caspase-3 and sensitize tumor cells to the action of gemcitabine and cisplatin (Cat. No. 232120), possibly by de-stabilizing p27. Preferentially increases cycling in Mirk-elevated quiescent pancreatic cancer cells (SU86.86, Panc1, AsPc1, and SW620 at ~1 µM). Also, shown to increase level of superoxides in quiescent pancreatic tumor cells (Panc1, SU86.86, and AsPc1) by blocking SOD2 and SOD3 activities.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₃H₁₇Cl₂N₅O₄
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (2 mg/ml)
          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
          ReferencesEwton, D.Z., et al. 2011. Mol. Cancer Ther. 10, 2104.