5.04981
Tie2/Trk Dual Inhibitor
Synonym(s):
Tie2/Trk Dual Inhibitor, Tie2 Inhibitor IV, Trk Inhibitor VII
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About This Item
Empirical Formula (Hill Notation):
C23H21ClN6O2
CAS Number:
Molecular Weight:
448.90
UNSPSC Code:
12352200
assay
≥99% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Secondary Target
Tie-2
Tie-2
Reversible: yes
Cell permeable: yes
Primary Target
TrkA
TrkA
Disclaimer
Toxicity: Standard Handling (A)
General 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.
Other Notes
Arcari, J.T., et al. 2013. Bioorg. Med. Chem. Lett.23, 3059.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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