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.

• Synonym(s): IGF-1R Inhibitor II, PQ401, N-(2-Methoxy-5-chlorophenyl)-Nʹ-(2-methylquinolin-4-yl)-urea, PQ401
• Empirical Formula (Hill Notation): C₁₈H₁₆ClN₃O₂
• CAS Number: 196868-63-0
• Molecular Weight: 341.79
• MDL number: MFCD00160558
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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
• storage temp.: 2-8°C
• 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

Description

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.

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable