533850 TAM Receptor Kinase Inhibitor, LDC1267 - CAS 1361030-48-9 - Calbiochem

533850
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₃₀H₂₆F₂N₄O₅ 1361030-48-9

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      5.33850.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable, bioactive, non-toxic quinoline based compound that acts as a highly potent, ATP-non-competitive, tight-binding type II TAM (Tyro3, Axl, and Mer) kinase inhibitor (IC50 = 8, 29, and 5 nM, respectively for Tyro3, Axl, and Mer). Occupies both the ATP binding cleft and an adjacent hydrophobic pocket. Also displays inhibitory activity against Met, Aurora B, Lck, and Src, but only at relatively higher concentration (IC50 = 35, 36, 51, and 338 nM, respectively). Displays modest selectivity over 39 other protein kinases (at ~1 µM). Reduces the proliferation of selected cancer lines (~ 15 µM). By inhibiting TAM receptors, it enhances anti-metastatic activity of natural killer (NK) cells via TAMR/E3 ligase (Cbl-b; casitas B-lineage lymphoma-b) pathway modulation. Reduces the number and size of 4T1 micro metastases in the liver of an orthotopic murine model of metastatic breast cancer without apparently affecting the primary mammary tumor. Also shown to reduce metastatic spreading of B16F10 melanomas, an effect that is abolished upon NK1.1 depletion.

          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 Number533850
          Brand Family Calbiochem®
          SynonymsTAM Receptor Blocker
          References
          ReferencesPaolino, M., et al. 2014. Nature. 507, 508.
          Product Information
          CAS number1361030-48-9
          FormWhite solid
          Hill FormulaC₃₀H₂₆F₂N₄O₅
          Chemical formulaC₃₀H₂₆F₂N₄O₅
          Applications
          Biological Information
          Primary TargetTyro3, Axl, and Mer kinases
          Primary Target IC<sub>50</sub>8, 29, and 5 nM for Tyro3, Axl, and Mer, respectively
          Secondary targetMet, Aurora B, Lck and Src kinases
          Purity≥98% by HPLC
          Physicochemical Information
          Cell permeableY
          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 for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          TAM Receptor Kinase Inhibitor, LDC1267 - CAS 1361030-48-9 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Paolino, M., et al. 2014. Nature. 507, 508.
          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.

          Revision20-November-2015 JSw
          SynonymsTAM Receptor Blocker
          DescriptionA cell-permeable, bioactive, non-toxic quinoline based compound that acts as a highly potent, ATP-non-competitive, tight-binding type II TAM (Tyro3, Axl, and Mer) kinase inhibitor (IC50 = 8, 29, and 5 nM, respectively for Tyro3, Axl, and Mer). Occupies both the ATP binding cleft and an adjacent hydrophobic pocket. Also displays inhibitory activity against Met, Aurora B, Lck, and Src, but only at relatively higher concentration (IC50 = 35, 36, 51, and 338 nM, respectively). Displays modest selectivity over 39 other protein kinases (at ~1 µM). Reduces the proliferation of selected cancer lines (~ 15 µM). By inhibiting TAM receptors, it enhances anti-metastatic activity of natural killer (NK) cells via TAMR/E3 ligase (Cbl-b; casitas B-lineage lymphoma-b) pathway modulation. Reduces the number and size of 4T1 micro metastases in the liver of an orthotopic murine model of metastatic breast cancer without apparently affecting the primary mammary tumor. Also shown to reduce metastatic spreading of B16F10 melanomas, an effect that is abolished upon NK1.1 depletion.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1361030-48-9
          Chemical formulaC₃₀H₂₆F₂N₄O₅
          Purity≥98% by HPLC
          SolubilityDMSO (50 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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesPaolino, M., et al. 2014. Nature. 507, 508.