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.
Synonym(s):
IGF-1R Inhibitor II, PQ401, N-(2-Methoxy-5-chlorophenyl)-Nʹ-(2-methylquinolin-4-yl)-urea, PQ401
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.
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, i.p.). The mechanism of inhibition probably involves indirect blocking of ATP binding.
Biochem/physiol Actions
Cell permeable: yes
Primary Target 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
Warning
Toxicity: Standard Handling (A)
Reconstitution
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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