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445835 Mer RTK Inhibitor, UNC569 - Calbiochem

445835
Purchase on Sigma-Aldrich

Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₂H₂₉FN₆

Products

Catalogue NumberPackaging Qty/Pack
445835-10MG Glass bottle 10 mg
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®
SynonymsMERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
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
Global Trade Item Number
Catalogue Number GTIN
445835-10MG 04055977204605

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
SynonymsMERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I, UNC-569, 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine
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 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 fo rup to 6 months at -20°C.
Toxicity Standard Handling
ReferencesLiu, J., et al. 2012. ACS Med. Chem. Lett. 3, 129.