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

TAM Receptor Kinase Inhibitor, LDC1267, is a cell-permeable, tight-binding "type II" TAM kinase inhibitor (IC₅₀ = 8, 29 & 5 nM for Tyro3, Axl & Mer). Enhances anti-metastatic activity of NK cells.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: TAM Receptor Blocker

Primary Target: Tyro3, Axl, and Mer kinases
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1361030-48-9C₃₀H₂₆F₂N₄O₅

Products

Catalogue NumberPackaging Qty/Pack
5.33850.0001 Glass bottle 10 mg
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
Quality LevelMQ100
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
Global Trade Item Number
Catalogue Number GTIN
5.33850.0001 04055977286755

Documentation

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

Title

Safety Data Sheet (SDS) 

TAM Receptor Kinase Inhibitor, LDC1267 - CAS 1361030-48-9 - Calbiochem Certificates of Analysis

TitleLot Number
533850

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 Protect from light
+2°C to +8°C
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.