Cellular Assay Services

Cellular Phosphorylation Assays / Cellular Kinase Assays

Field of Application

Our cellular kinase assays have been designed to measure compound activity in a physiological environment on a physiological substrate. Cellular kinase assays are therefore a crucial part of rationale drug development.

Our Service

Select Phosphorylation Assays

#

Kinase

Cell Line

Reference Compound

Info Sheet

1

AKT1 (h)

Rat1-myrAKT1 (r)

Staurosporine

2

ALK (h)

Karpas-299 (h)

Crizotinib (Xalkori®)

3

Aurora-B (h)

HT-29 (h)

Staurosporine

4

AXL (h)

MEF-AXL (m)

Sunitinib (Sutent®)

5

BCR-ABL

K562

Dasatinib (Sprycel®)

6

B-RAF-VE (h)

Rat1-B-RAF-VE (r)

Sorafenib (Nexavar®)

7

EGF-R (h)

A431 (h)

Lapatinib (Tyverb®)

8

EGF-R G719S Mutant (h)

Rat1 (r)

Lapatinib (Tyverb®)

9

EGF-R L858R Mutant (h)

Rat1 (r)

Lapatinib (Tyverb®)

10

EGF-R L861Q Mutant (h)

Rat1 (r)

Lapatinib (Tyverb®)

11

EGF-R T790M Mutant (h)

Rat1 (r)

Staurosporine

12

EGF-R T790M/L858R Mutant (h)

Rat1 (r)

Staurosporine

17

EGF-R Δ752-759 Mutant (h)

Rat1 (r)

Lapatinib (Tyverb®)

16

EGF-R Δ747-749/A750P Mutant (h)

Rat1 (r)

Lapatinib (Tyverb®)

19

EGF-R control wt (h)

Rat1 (r)

Lapatinib (Tyverb®)

20

EPHB4 (h)

MEF-EPHB4 (m)

Sorafenib (Nexavar®)

21

ERBB2 (h)

NIH3T3-ERBB2 (m)

Lapatinib (Tyverb®)

22

ERBB4 (h)

T47D (h)

Lapatinib (Tyverb®)

23

FAK (h)

MEF-FAK (m)

Staurosporine

24

FGF-R2

Kato III

Nintedanib (Vargatef®)

25

FLT3-wt (h)

MEF-FLT3-wt (m)

Sunitinib (Sutent®)

26

FLT3-DY (h)

MEF-FLT3-DY (m)

Sunitinib (Sutent®)

27

FLT3-ITD (h)

MEF-FLT3-ITD (m)

Sunitinib (Sutent®)

28

FYN (h)

Rat1 (r)

Dasatinib (Sprycel®)

29

Haspin (GSG2)

HT-29 (h)

CHR 6494

30

IGF1-R (h)

MEF-IGF1-R (m)

Staurosporine

31

KIT (h)

M07e (h)

Sunitinib (Sutent®)

32

MET (h)

MKN45 (h)

PHA665752

33

MET D1228H Mutant (h)

Rat1 (r)

BMS777607

34

MET D1228N Mutant (h)

Rat1 (r)

BMS777607

35

MET F1200l Mutant (h)

Rat1 (r)

BMS777607

36

MET M1250T Mutant (h)

Rat1 (r)

BMS777607

37

MET Y1230A Mutant (h)

Rat1 (r)

BMS777607

38

MET Y1230C Mutant (h)

Rat1 (r)

BMS777607

39

MET Y1230D Mutant (h)

Rat1 (r)

BMS777607

40

MET Y1230H Mutant (h)

Rat1 (r)

BMS777607

41

MET control wt (h)

Rat1 (r)

BMS777607

42

MNK1 (h)

Karpas-299 (h)

CGP 57380

43

PDGFR-beta (m)

NIH3T3 (m)

Sunitinib (Sutent®)

44

PIM1

HEK293T (h)

AZD1208

45

PIM2

HEK293T (h)

AZD1208

46

PIM3

HEK293T (h)

AZD1208

47

ROCK (r)

A7r5 (r)

Y27632

48

RON (h)

T47D (h)

Crizotinib (Xalkori®)

49

S6K (h)

Karpas-299 (h)

Everolimus (Afinitor®)

50

SRC (h)

MEF-SRC (m)

Dasatinib (Sprycel®)

51

TIE2 (h)

CHO-TIE2 (ha)

Sorafenib (Nexavar®)

52

VEGF-R2 (h)

HUE (h)

Sunitinib (Sutent®)

53

VEGF-R3 (h)

MEF-VEGF-R3 (m)

Sunitinib (Sutent®)

13

EGF-R Δ746-750/C797S Mutant (h)

Rat1 (r)

Staurosporine

14

EGF-R Δ746-750/T790M Mutant (h)

Rat1 (r)

Staurosporine

15

EGF-R Δ746-750/T790M/C797S Mutant (h)

Rat1 (r)

Staurosporine

18

EGF-R T790M/C797S/L858R Mutant (h)

Rat (r)

Staurosporine

origin of kinase and cell line: (h) = human, (m) = mouse, (r) = rat, (ha) = hamster

Info in Brief

Cpd Exposure

90 min

Readout

ELISA (sandwich or solid phase)

Testing Formats

IC50 (8 semi-log dilutions in duplicate)

Cpd Submission

Solved or as pre-weighed powder

Tolerable Solvent

Max 1 % DMSO

Report

Comprehensive evaluation of data including raw data for own analysis
Sample report will be provided upon request

Summary Sheet

PDF

List of Kinases for this Service

PDF

Guidelines for Cpd Submission

EXCEL-FILE

Other compounds tested in our cellular phosphorylation assays

Afatinib (Giotrif®), AZD4547, Bosutinib (SKI-606), Imatinib (Glivec®), Infigratinib (BGJ-398), Nazartinib (EGF-816), Nilotinib (Tasigna®), Osimertinib (Tagrisso®), PF-06747775, Ponatinib (AP-24534), Quizartinib, Saracatinib (AZD-0530), SGI-1776, Tozasertib (MK-0457, VX-680), Vatalanib (PTK787)