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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C18H16ClN3O2
CAS Number:
196868-63-0
Molecular Weight:
341.79
UNSPSC Code:
12352200
MDL number:
MFCD00160558

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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

100

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
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)

Storage Class

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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