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Description
Overview
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 Number
504981
Brand Family
Calbiochem®
Synonyms
Tie2 Inhibitor IV, Trk Inhibitor VII
References
References
Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett.23, 3059.
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.
Revision
20-September-2013 JSW
Synonyms
Tie2 Inhibitor IV, Trk Inhibitor VII
Description
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, 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.
Form
White solid
Intert gas (Yes/No)
Packaged under inert gas
Chemical formula
C₂₃H₂₁ClN₆O₂
Structure formula
Purity
≥99% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity
Standard Handling
References
Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett.23, 3059.
