445835 Mer RTK Inhibitor, UNC569 - Calbiochem

445835
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₂H₂₉FN₆

Pricing & Availability

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445835-10MG
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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
      Quality LevelMQ100
      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

      Mer RTK Inhibitor, UNC569 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Mer RTK Inhibitor, UNC569 - Calbiochem 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.