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504981 Tie2/Trk Dual Inhibitor - Calbiochem

Tie2/Trk Dual Inhibitor - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Tie2 Inhibitor IV, Trk Inhibitor VII

Primary Target: TrkA
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₂₁ClN₆O₂
Description
Overview

This product has been discontinued.



A cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC50 = 40 and 0.4 nM, respectively; [ATP] = 100 µM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC50 = 3.7 and 4 nM, with respective NIH 3T3 transfectant), displaying much reduced potency against PDGFR (IC50 =1.4 µM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >10 µM). Reported to be efficacious in suppressing rat C6 glioblastoma tumor expansion (10 to 33 mg/kg/d, or 10 mg/kg/12 h p.o.) in vivo.
Catalogue Number504981
Brand Family Calbiochem®
SynonymsTie2 Inhibitor IV, Trk Inhibitor VII
References
ReferencesArcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.
Product Information
FormWhite solid
Hill FormulaC₂₃H₂₁ClN₆O₂
Chemical formulaC₂₃H₂₁ClN₆O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetTrkA
Secondary targetTie-2
Purity≥99% 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 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
504981 0

Documentation

Tie2/Trk Dual Inhibitor - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.
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-September-2013 JSW
SynonymsTie2 Inhibitor IV, Trk Inhibitor VII
DescriptionA cell-permeable pyrrolopyrimidinyl-phenyl urea that acts as a potent, reversible, ATP-competitive inhibitor against Tie2 and TrkA kinase activity in cell-free assays (IC50 = 40 and 0.4 nM, respectively; [ATP] = 100 µM) as well as Tie2- and TrkA-dependent tyrosine phosphorylation of cellular proteins upon ligand stimulation in cultures (IC50 = 3.7 and 4 nM, respectively, using respective NIH 3T3 transfectant; 1 h drug preincubation), displaying much reduced potency against PDGFR (IC50 =1.4 µM) and little or no inhibitory activity toward EGFR, FGFR, or KDR (IC50 >10 µM). Reported to be orally available in rat (systemic Cmax = 1,715 ng/mL; Tmax = 0.75 h; 4.2 mg/kg p.o. using ultrafasted rats) and efficacious in suppressing rat C6 glioblastoma tumor expansion (by 40%, 60%, and 70% in 10 d, respectively, with 10 mg/kg/d, 33 mg/kg/d, or 10 mg/kg/12 h oral dosing schedule) in vivo.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₃H₂₁ClN₆O₂
Structure formulaStructure formula
Purity≥99% 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 6 months at -20°C.
Toxicity Standard Handling
ReferencesArcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett. 23, 3059.