in vitro PHARMACOLOGY 2011 CATALOG - Cerep

116 in vitro pharmacology 2011 catalog
❚ protein-tyrosine kinases [Rtk]
PDGFRb kinase
Ref. 2900
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(25 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 1 nM)
Baxter, R.M. et al. (1998) J. Biol. Chem., 273: 17050-17055.
Ret kinase
Ref. 1593
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + biotinyl-bAbAbAAEEEEYFELVAKKK
(100 nM)
Measured product phospho-biotinyl-bAbAbAAEEEEYFELVAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 8 nM)
Borrello, M.G. et al. (1996) Mol. Cell. Biol., 16: 2151-2163.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100
50
staurosporine
SU4312
SU4984
0
PD153035
-10 -9 -8 -7 -6 -5 -4
-11
log [drug] (M)
Ron kinase
Ref. 3067
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-TK peptide
(20 nM)
Measured product phospho-Ulight-TK peptide
Detection method LANCE
Reference
staurosporine (IC 50 : 470 nM)
Santoro, M.M. et al. (1998) Oncogene, 17: 741-749.
-10 -9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -9 -4
-9 -8 -7 -6 -5 -4
-8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
PD153035
staurosporine
AG1478
AG825
Ros kinase
Ref. 1594
Q 3 weeks
Included in:
Comprehensive kinase profile
Source
human recombinant (Sf21 cells)
Substrate
ATP + biotinyl-bAbAbAAAEEEYMMMFAKKK
(75 nM)
Measured product phospho-biotinyl-bAbAbAAAEEEYMMFAKKK
Detection method HTRF
Reference
staurosporine (IC 50 : 7.6 nM)
Birchmeier C. et al. (1990) Proc. Natl. Acad. Sci. USA, 87: 4799-4803.
-9 -8 -7 -6 -5 -4
enzyme activity (% of control)
100
50
staurosporine
PD153035
0
K252a
-9 -8 -7 -6 -5 -4
-10
log [drug] (M)
-11 -10 -9 -8 -7 -6 -5 -4
TIE2 kinase
Ref. 2736
Q 3 weeks
Included in:
Organ safety profile
Comprehensive kinase profile
Source
human recombinant
Substrate
ATP + Ulight-Poly GT [EY(4:1)]n
(50 nM)
Measured product phospho-Ulight-Poly GT [EY(4:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 260 nM)
Deng, S-J. et al. (2001) Comb. Chem. High Throughput Screen., 4: 525-533.
-10 -9 -8 -7 -6 -5 -4
-9 -8 -7 -6 -5 -4
-4
-9 -8 -7 -6 -5
-8 -7 -6 -5 -4
-11 -10 -9 -8 -7 -6 -5 -4
PD153035
staurosporine
AG1478
AG825
TRKA
Ref. 2901
Q 3 weeks
Included in:
ExpresS Diversity kinase profile
Organ safety profile
Comprehensive kinase profile
Source
human recombinant (insect cells)
Substrate
ATP + Ulight-Poly GAT[EAY(1:1:1)]n
(5 nM)
Measured product phospho-Ulight-Poly GAT[EAY(1:1:1)]n
Detection method LANCE
Reference
staurosporine (IC 50 : 5.5 nM)
Angeles, T.S. et al. (1998) Arch. Biochem. Biophys., 349: 267-274.