Ret (V804M) Human RTK Kinase Enzymatic Radiometric [Km ATP] KinaseProfiler LeadHunter Assay - FR

Item: 14-760KP

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Status: Available

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

The RET (rearranged during transfection) receptor tyrosine kinase is a classic example of phenotype heterogeneity. Gain-of-function mutations of RET are associated with human cancer and multiple endocrine neoplasia type 2 (MEN 2A, MEN 2B, etc.) Loss-of-function mutations of RET cause Hirschspung disease or colonic aganglionosis).

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

Ret

Uniprot Number:

P07949

Protein Aliases:

cadherin-related family member 16|RET receptor tyrosine kinase|rearranged during transfection

Gene Name:

RET

Gene ID:

5979

Gene Aliases:

PTC|CDHF12|RET51|CDHR16

Accession Number:

NM_000323

Organism:

Human

Construct Details:

658-end; V804M recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Ret (V804M) (h) is incubated with 8 mM MOPS pH 7.0, 0.2 mM EDTA, 100 mM NaCl, 100 µM KKKVSRSGLYRSPSMPENLNRPR, 10 mM MgAcetate and [gamma-33P]-ATP (specific activity and concentration as required). The reaction is initiated by the addition of the Mg/ATP mix. After incubation for 40 minutes at room temperature, the reaction is stopped by the addition of phosphoric acid to a concentration of 0.5%. An aliquot of the reaction is then spotted onto a filter and washed four times for 4 minutes in 0.425% phosphoric acid and once in methanol prior to drying and scintillation counting.

Substrate:

100 µM KKKVSRSGLYRSPSMPENLNRPR

Tracer:

33P

ATP Concentration:

[ATP]= 45µM (Km= 42.5µM )

Incubation:

40 min at Room temperature

Control Inhibitor:

Staurosporine

Test Sample Requirements:

Please provide compounds dissolved in 100% DMSO (PBS or HBSS prohibited).
Stock solution should be ≥50× the final assay concentration (a 10 mM stock is also acceptable).
Required volume:
– <60 kinase assays: 120 µL of 50× stock
– ≥60 assays: 420 µL of 50× stock
If you supply 10 mM stocks or powder (pre-weighed), we will apply the appropriate conversion.
For batches of ~50 compounds supplied as solids, the TAT will be extended.

Minimum Order Quantity:

Turnaround Time

Standard:

6 Business Days

Service Scheduling Note:

Assay is run on a weekly schedule beginning on Friday. Compounds and purchase order must be received on or before 13:00 CET Thursday for the order to be included on the service run that begins on Friday of the same week.

Reference Compound Data

PubChem ID

122130844

Name

Staurosporine

Measurement

2.78nM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Adverse / Beneficial Action:

Inhibition of RET may be useful in the treatment of multiple endocrine cancers.

Additional Information

Brand:

LeadHunter

Testing Location:

KP - France - Celle L'Evescault