in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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110 <strong>in</strong> <strong>vitro</strong> pharmacology <strong>2011</strong> catalog<br />
❚ prote<strong>in</strong>-tyros<strong>in</strong>e k<strong>in</strong>ases [Rtk]<br />
EphA1 k<strong>in</strong>ase<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + biot<strong>in</strong>yl-bAbAbAAEEEIYEEIEAKKK<br />
(100 nM)<br />
Ref. 1873<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAAEEEIYEEIEAKKK<br />
Detection method HTRF<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 140 nM)<br />
Comprehensive k<strong>in</strong>ase profile Coulthard, M.G. et al. (2001) Growth Factors, 18: 303-317.<br />
enzyme activity (% of control)<br />
100<br />
50<br />
0<br />
-9 -8 -7 -6 -5 -4<br />
log [drug] (M)<br />
staurospor<strong>in</strong>e<br />
PP1<br />
PP2<br />
PD153035<br />
EphA2 k<strong>in</strong>ase<br />
Ref. 3055<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
Measured product<br />
Detection method<br />
Reference<br />
-11<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
-9 -8 -7 -6 -5 -4<br />
-10<br />
ATP + Ulight-TK peptide<br />
(50 nM)<br />
phospho-Ulight-TK peptide<br />
LANCE<br />
staurospor<strong>in</strong>e (IC 50 : 150 nM)<br />
K<strong>in</strong>ch, M.S. et al. (2003) Cl<strong>in</strong>. Cancer Res., 9: 613-618.<br />
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<br />
-10 -9 -8 -7 -6 -5 -4 -3<br />
-8 -7 -6 -5 -4<br />
-10 -9 -8 -7 -6 -5<br />
<br />
-10 -9 -8 -7 -6 -5 -4<br />
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EphA3 k<strong>in</strong>ase<br />
Ref. 3066<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
ExpresS Diversity k<strong>in</strong>ase profile<br />
Comprehensive k<strong>in</strong>ase profile<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
ATP + Ulight-TK peptide<br />
(50 nM)<br />
Measured product phospho-Ulight-TK peptide<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 57.5 nM)<br />
Sharfe, N. et al. (2003) J. Immunol., 170: 6024-6032.<br />
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EphA4 k<strong>in</strong>ase<br />
Ref. 1702<br />
Q 3 weeks<br />
Included <strong>in</strong>:<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 + biot<strong>in</strong>yl-βAβAβAAEEEIYEEIEAKKK<br />
(400 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-βAβAβAAEEEIYEEIEAKKK<br />
Detection method HTRF<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 150 nM)<br />
B<strong>in</strong>ns, K.L. et al. (2000) Mol. Cell. Biol., 20: 4791-4805.<br />
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EphA5 k<strong>in</strong>ase<br />
Ref. 2640<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 />
(5 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 : 60 nM)<br />
B<strong>in</strong>ns, K.L. et al. (2000) Mol. Cell. Biol., 20: 4791-4805.<br />
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EphA6 k<strong>in</strong>ase<br />
Ref. 3071<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
ATP + Ulight-TK peptide<br />
(100 nM)<br />
Measured product phospho-Ulight-TK peptide<br />
Detection method LANCE<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 28.3 nM)<br />
Hafner, C. et al. (2004) Cl<strong>in</strong>. Cell., 50: 490-499.
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