Biochemical Assay Services

Standardized Kinase Profiling Packages

Field of Application

The standardized profiling service packages can be used for the characterization of your test compounds against different kinase panels. Depending on the package type compounds will either be tested with two data points for each kinase (1 conc in duplicate or 2 conc in singlicate) or at 6 or 10 concentrations with subsequent calculation of IC50 values.

Our Service

Broad Kinase Panel Selectivity Profiling

#

Type of Package

No. of Kinases

Data Points per Kinase

Description

Info Sheet

1

WildType IC50-Profiler

320

6 conc in singlicate

wildtype forms of protein kinases

2

WildType 2Point-Profiler

320

1 conc in duplicate or 2 conc in singlicate

wildtype forms of protein kinases

3

WildType+ 2Point-Profiler

410

1 conc in duplicate or 2 conc in singlicate

410 different kinases, including 79 disease relevant kinases & 13 lipid kinases

CDK IC50-Profiler

#

Type of Package

No. of Kinases

Data Points per Kinase

Reference Compound

Info Sheet

1

CDK IC50-Profiler

28

10 conc in singlicate

To be selected

Mutant IC50-Profiler

#

Type of Package

No. of Kinases

Data Points per Kinase

Reference Compound

Info Sheet

1

ABL1 Mutant IC50-Profiler

9

10 conc in singlicate

Imatinib (Gleevec®)

2

ALK Mutant IC50-Profiler

8

10 conc in singlicate

Crizotinib (Xalkori®)

3

EGF-R Mutant IC50-Profiler

11

10 conc in singlicate

Gefitinib (Iressa®)

4

KIT Mutant IC50-Profiler

10

10 conc in singlicate

Imatinib (Gleevec®)

5

MET Mutant IC50-Profiler

10

10 conc in singlicate

PHA665752

6

RET Mutant IC50-Profiler

10

10 conc in singlicate

BIBF1120 (Vargatef®)

Infos in Brief

Slots in 2018 for Broad Panel Profiling

Testing will start on:  January 08 // February 12 // March 12 // April 09 // May 07 // June 04 // July 02 // September 03 // October 01 // November 05 // December 03

No of Test Cpds in the Standard Packages

Broad Panel Profiler: 1 cpd; CDK-Profiler: 4 cpds; Mutant-Profiler: 1 cpd

Assay Technologies

Protein kinases: FlashPlate™-based radiometric assay; lipid kinases: ADP-Glo™ assay technology (Promega)

ATP conc

App. ATP-Km for each kinase

Cpd Submission

100 x Stock solution in 100 % DMSO or
pre-weighed powder (request guidelines)

Report

Detailed report for each project

Turnaround Time

Routinely within 10 working days

Info Sheets

Method: Radiometric Assay, Method: ADP-Glo™ Assay, List of WildType Profiler Kinases, List of WildType+ Profiler Kinases

Related Publication from ProQinase

ProQinase Poster from AACR meeting 2018, Chicago