PRALSETINIB

PRALSETINIB : Inhibitor of RET

Structure

SERP Rating

Probe PRALSETINIB is in the process of SERP review.

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Information

RET (Mutant:WT, V804M, M918T)

Inhibitor

up to 1 uM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P07949

Target Class: Kinase

Target SubClass: Tyrosine Kinase

Potency: IC50

Potency Value: 0.78 nM

Potency Assay: In Vitro Biochemical Activity Assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Proto-oncogene tyrosine-protein kinase receptor Re ...

DOI Reference: 10.1016/j.bmcl.2021.128149

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): BLU-667 was profiled against a panel of 106 kinases at Reaction biology. Kinase activity data were expressed as the percent remaining kinase activity in test samples compared to vehicle (dimethyl sulfoxide) reactions at 300 nM. Radioligand assay: JAK2 IC50 2.0 nM FLT3 IC50 6.5 nM

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