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Cellular Phosphorylation Assays |
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Advantages of Cellular Kinase Activity Assays
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cell permeability
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physiological environment
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inhibitor identification regardless of binding mode
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physiological substrate
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wild type and mutant kinases
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 Influences addressed in cellular phosphorylation assays |
Test systems
| Kinase Name |
Cell Line |
Trans-fected |
Fact
Sheet |
Type of Kinase |
| AKT1 (h) |
Rat1-myrAKT1 (r) |
yes |
|
Ser/Thr Kinase |
| ALK (h) |
Karpas-299 (h) |
no |
|
RTK |
| Aurora-B (h) |
HT-29 (h) |
no |
|
Ser/Thr Kinase |
| AXL (h) |
MEF-AXL (m) |
yes |
|
RTK |
| BCR-ABL (h) |
K562 |
no |
|
RTK |
| B-RAF-VE (h) |
Rat1-B-RAF-VE (r) |
yes |
|
Ser/Thr Kinase |
| EGF-R (h) |
A431 (h) |
no |
|
RTK |
| EPHB4 (h) |
MEF-EPHB4 (m) |
yes |
|
RTK |
| ERBB2 (h) |
NIH3T3-ERBB2 (m) |
yes |
|
RTK |
| FAK (h) |
MEF-FAK (m) |
yes |
|
Non-receptor TK |
| FGF-R2 (h) |
Kato-III |
no |
|
RTK |
| FLT3-wt (h) |
MEF-FLT3-wt (m) |
yes |
|
RTK |
| FLT3-DY (h) |
MEF-FLT3-DY (m) |
yes |
|
RTK |
| FLT3-ITD (h) |
MEF-FLT3-ITD (m) |
yes |
|
RTK |
| IGF1-R (h) |
MEF-IGF1-R (m) |
yes |
|
RTK |
| KIT (h) |
M07e (h) |
no |
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RTK |
| MET (h) |
MKN45 (h) |
no |
|
RTK |
| MET Mutant Panel (h) |
Rat1 (r) |
yes |
|
RTK |
| PDGFR-beta (m) |
NIH3T3 (m) |
no |
|
RTK |
| ROCK (r) |
A7r5 (r) |
no |
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Ser/Thr Kinase |
| S6K (h) |
Karpas-299 (h) |
no |
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Ser/ Thr Kinase |
| SRC (h) |
MEF-SRC (m) |
yes |
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Non-receptor TK |
| TIE2 (h) |
CHO-TIE2 (ha) |
yes |
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RTK |
| VEGF-R2 (h) |
HUE (h) |
no |
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RTK |
| VEGF-R3 (h) |
MEF-VEGF-R3 (m) |
yes |
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RTK |
Study example
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In a comprehensive study, clinical kinase inhibitors were tested in cellular phosphorylation assays on 17 oncologically relevant kinases (more details, see on our poster "profiling of kinase inhibitors"). As an example out of this study the IC50 curves for Sunitinib on EPHB4, FLT3-wt, TIE2, and VEGF-R2 phosphorylation are demonstrated with IC50 values of >10µM (EPHB4), 25nM (FLT3-wt), >10µM (TIE2), and 9.1nM (VEGF-R2) . |
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IC50 determination of Sunitinib on EPHB4,
FLT3-wt, TIE2 and VEGF-R2 phosphorylation
[click here to enlarge image]
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Our service
ProQinase offers analysis of test compounds in the cellular phosphorylation assay either as single concentration measurement (in duplicate) or as IC50 determination based on 8 semi-log diluted concentrations. The service is available for all kinases wich are listed in the table above. Further assays can be established according to your specific requirements.
Please inquire to receive a custom-tailored quote according to your individual requirements.
Related assays:
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