in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
in vitro PHARMACOLOGY 2011 CATALOG - Cerep
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113<br />
FLT-3 k<strong>in</strong>ase<br />
Ref. 2866<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 (<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 />
staurospor<strong>in</strong>e (IC 50 : 0.67 nM)<br />
Dosil, M. et al. (1993) Mol. Cell. Biol., 13: 6572-6585.<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 />
FLT-3 D835Y k<strong>in</strong>ase<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + Ulight-TK peptide (50 nM)<br />
Measured product phospho-Ulight-TK-peptide<br />
Detection method LANCE<br />
Ref. 3208<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 0.7 nM)<br />
Q 3 weeks<br />
Zhang, W. et al.(2008) J. Natl. Cancer Inst., 100: 184-198.<br />
FLT-4 k<strong>in</strong>ase (VEGFR3)<br />
Source<br />
human recomb<strong>in</strong>ant<br />
Substrate<br />
ATP + Ulight-CAGAGAIETDKEYYTVKD<br />
(100 nM)<br />
Measured product phospho-Ulight-CAGAGAIETDKEYYTVKD<br />
Ref. 2896<br />
Detection method LANCE<br />
Q 3 weeks<br />
Included <strong>in</strong>:<br />
Reference<br />
staurospor<strong>in</strong>e (IC 50 : 2.3 nM)<br />
Comprehensive k<strong>in</strong>ase profile Kirk<strong>in</strong>, V. et al. (2001) Eur. J. Biochem., 268: 5530-5540.<br />
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Ion<br />
channels<br />
Transporters<br />
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K<strong>in</strong>ases<br />
Epigenetic &<br />
DNA-related<br />
enzymes<br />
Fms/CSFR k<strong>in</strong>ase<br />
Ref. 3069<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-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 : 0.95 nM)<br />
Carlberg, K. and Rohrschneider, L. (1994) Mol. Cell. Biol., 5: 81-95.<br />
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Other<br />
enzymes<br />
Specialized<br />
cellular<br />
assays<br />
HER2/ErbB2 k<strong>in</strong>ase<br />
Ref. 1598<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-bAbAbAAEEEEYFELVAKKK<br />
(600 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAAEEEEYFELVAKKK<br />
Detection method HTRF<br />
Reference<br />
PD153035 (IC 50 : 1.8 µM)<br />
Qian, X. et al. (1992) Proc. Natl. Acad. Sci. USA, 89: 1330-1334.<br />
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Standard<br />
profiles<br />
Test<strong>in</strong>g<br />
conditions<br />
HER4/ErbB4 k<strong>in</strong>ase<br />
Ref. 1875<br />
Q 3 weeks<br />
Source<br />
human recomb<strong>in</strong>ant (<strong>in</strong>sect cells)<br />
Substrate<br />
ATP + biot<strong>in</strong>yl-bAbAbAAEEEEYFELVAKKK<br />
(25 nM)<br />
Measured product phospho-biot<strong>in</strong>yl-bAbAbAAEEEEYFELVAKKK<br />
Detection method HTRF<br />
Reference<br />
PD153035 (IC 50 : 300 nM)<br />
Plowman, G.D. et al. (1993) Proc. Natl. Acad. Sci. USA, 90: 1746-1750.<br />
enzyme activity (% of control)<br />
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100<br />
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50<br />
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0<br />
-9 -8 -7 -6 -5 -4<br />
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log [drug] (M)<br />
PD153035<br />
staurospor<strong>in</strong>e<br />
Order<strong>in</strong>g<br />
<strong>in</strong>formation<br />
Assay list<br />
& <strong>in</strong>dex<br />
-11<br />
-10 -9 -8 -7 -6 -5 -4<br />
-3<br />
-10<br />
-9 -8 -7 -6 -5 -4<br />
-3<br />
-9 -8 -7 -6 -5 -4 -8 -7 -6 -5 -4
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