BLU-654

BLU-654 : Inhibitor of KIT

Structure

SERP Rating

Probe BLU-654 is in the process of SERP review.

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Information

KIT (Mutant:WT, V654A)

Inhibitor

up to 1 uM

In Vitro Validations

Uniprot ID: P10721

Target Class: Kinase

Target SubClass: Tyr kinase

Potency: Kd

Potency Value: 0.4 nM

Potency Assay: DiscoverX assay for KIT(V559D,V654A)

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

Target aliases:

Mast/stem cell growth factor receptor Kit, KIT, KI ...

DOI Reference: 10.1021/acs.jmedchem.5c03554

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): DiscoverX KINOMEScan selectivity profiling at 3 μM

Probe Selectivity in Vitro:

BLU-654 exibiterd substantial selectivity margin over WT (15-fold) and PDGFRβ (219-fold) and exhibited a favorable kinome selectivity profile with an S(10) of 0.06.

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SERP ratings and comments

No SERP comments found for BLU-654