445835 | Mer RTK Inhibitor, UNC569 - Calbiochem

445835
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₉FN₆

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      445835-10MG
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      Limited AvailabilityLimited Availability
      Stocked 
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      Available
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          Glass bottle 10 mg
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          Description
          OverviewAn orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC50 = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC50 of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.
          Catalogue Number445835
          Brand Family Calbiochem®
          Synonyms1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569
          References
          ReferencesLiu, J., et al. 2012. ACS Med. Chem. Lett. 3, 129.
          Product Information
          FormBeige powder
          FormulationSupplied as a trifluoroacetate salt.
          Hill FormulaC₂₂H₂₉FN₆
          Chemical formulaC₂₂H₂₉FN₆
          Structure formula ImageStructure formula Image
          Applications
          ApplicationMer RTK Inhibitor, UNC569, 1350547-65-7 is a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM).
          Biological Information
          Purity≥95% 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 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 fo rup 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
          445835

          References

          Reference overview
          Liu, J., et al. 2012. ACS Med. Chem. Lett. 3, 129.
          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.

          Revision28-August-2017 JSW
          Synonyms1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569
          DescriptionAn orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50 = 2.9 nM; Ki = 4.3 nM) with ~10-fold greater selectivity over other TAM family kinases (IC50 = 37 and 48 nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30 nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC50 of 141 nM. Exhibits desirable pharmacokinetic profile and efficacy in mice.
          FormBeige powder
          FormulationSupplied as a trifluoroacetate salt.
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₂₉FN₆
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml) or H₂O (2.5 mg/ml with gentle warming)
          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 fo rup to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesLiu, J., et al. 2012. ACS Med. Chem. Lett. 3, 129.