407248
IGF-1R Inhibitor II, PQ401
The IGF-1R Inhibitor II, also referenced under CAS 196868-63-0, controls the biological activity of IGF-1R. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
别名:
IGF-1R Inhibitor II, PQ401, N-(2-Methoxy-5-chlorophenyl)-Nʹ-(2-methylquinolin-4-yl)-urea, PQ401
InChI
1S/C18H16ClN3O2/c1-11-9-15(13-5-3-4-6-14(13)20-11)21-18(23)22-16-10-12(19)7-8-17(16)24-2/h3-10H,1-2H3,(H2,20,21,22,23)
InChI key
YBLWOZUPHDKFOT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 10 mg/mL, ethanol: 3 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable phenylquinolinyl-urea compound that inhibits IGF-1R autophosphorylation (IC50 = 12 µM in inhibiting ligand-induced autophosphorylation in MCF-7 cells and <1 µM in a cell-free kinase assay). Reduces IGF-1R-dependent tumor cell growth both in vitro (IC50 = 8 and 15 µM for MCF-7 and MCNeuA, respectively) and in mice in vivo (80% reduction, 100 mg/kg thrice a week per i.p.). The mechanism of inhibition probably involves indirect blocking of ATP binding.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
IGF-1R
IGF-1R
Product does not compete with ATP.
Reversible: no
Target IC50: 12 µM in inhibiting ligand-induced IGF-1R autophosphorylation in MCF-7 cells and <1 µM in a cell-free kinase assay; 8 and 15 µM in reducing IGF-1R-dependent tumor cell growth both in vitro for MCF-7 and MCNeuA, respectively
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.
Other Notes
Gable, K.L., et al. 2006. Mol. Cancer Ther.5, 1079.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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