in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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109<br />
DDR2 k<strong>in</strong>ase<br />
Ref. 2783<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
ATP + Ulight-Poly GAT[EAY(1:1:1)]n<br />
(50 nM)<br />
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 3.1 nM)<br />
Vogel, W. (1999) FASEB J., 13: S77-82.<br />
prote<strong>in</strong>-tyros<strong>in</strong>e k<strong>in</strong>ases [Rtk] ❚<br />
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<strong>Cerep</strong><br />
services<br />
Receptors<br />
EGFR k<strong>in</strong>ase<br />
Ref. 2865<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
Organ safety profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + Ulight-CAGAGAIETDKEYYTVKD<br />
(100 nM)<br />
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD<br />
Detection method LANCE<br />
Reference<br />
PD153035 (IC 50 : 0.21 nM)<br />
Weber, W. et al. (1984) J. Biol. Chem., 259: 14631-14636.<br />
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Ion<br />
channels<br />
Transporters<br />
EGFR k<strong>in</strong>ase (A431 cells) - AlphaScreen<br />
cellul ar<br />
Ref. 3100<br />
Ref. 3105<br />
Q 3 weeks<br />
Activator effect<br />
Inhibitor effect<br />
Source<br />
A431 cells<br />
Measured product phosphorylation<br />
Detection method AlphaScreen<br />
Activator effect Control EGF (1 µM)<br />
Reference EGF (EC 50 : 17.2 nM)<br />
Inhibitor effect Stimulant EGF (300 nM)<br />
Reference AG1478 (IC 50 : 3.1 nM)<br />
Zhang, Y.G. et al.(2008) Int. J. Oncol., 33: 595-602.<br />
EGFR k<strong>in</strong>ase (A431 cells) - impedance<br />
cellul ar<br />
Ref. 3210<br />
Ref. 3215<br />
Q 3 weeks<br />
Activator effect<br />
Inhibitor effect<br />
EGFR k<strong>in</strong>ase (Hela cells)<br />
cellul ar<br />
Ref. 3209<br />
Ref. 3212<br />
Q 3 weeks<br />
Activator effect<br />
Inhibitor effect<br />
Source<br />
A431 cells<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Activator effect Control EGF (100 nM)<br />
Reference EGF (EC 50 : 0.3 nM)<br />
Inhibitor effect Stimulant EGF (3 nM)<br />
Reference AG1478 (IC 50 : 124 nM)<br />
Kondratov, K.A. et al.(2009) Cell. Biol. Int., 34: 81-87.<br />
Source<br />
EGFR k<strong>in</strong>ase (MDA-MB-231 cells)<br />
cellul ar<br />
Ref. 3211<br />
Ref. 3214<br />
Q 3 weeks<br />
Activator effect<br />
Inhibitor effect<br />
Hela cells<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Activator effect Control EGF (1 nM)<br />
Reference EGF (EC 50 : 0.033 nM)<br />
Inhibitor effect Stimulant EGF (0.1 nM)<br />
Reference AG1478 (IC 50 : 21 nM)<br />
Abulrob, A. et al. (2010) J. Biol. Chem., 285: 3145-3156.<br />
Source<br />
MDA-MB-231 cells<br />
Measured product impedance<br />
Detection method cellular dielectric spectroscopy<br />
Activator effect Control EGF (10 nM)<br />
Reference EGF (EC 50 : 0.16 nM)<br />
Inhibitor effect Stimulant EGF (1 nM)<br />
Reference AG1478 (IC 50 : 47 nM)<br />
Amor<strong>in</strong>o, G.P., et al. (2002) Mol. Biol. Cell., 13: 2233-2344<br />
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[Solvent] must be kept 0.3%<br />
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[Solvent] must be kept 0.3%<br />
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[Solvent] must be kept 0.1%<br />
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[Solvent] must be kept 0.1%<br />
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K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex
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