Vimseltinib

Inhibitor of CSF1R

Structure

SERP Rating

Probe Vimseltinib is in the process of SERP review.

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Information

CSF1R

Inhibitor

1 µM

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: P07333

Target Class: Kinase

Target SubClass: TK

Potency: IC50

Potency Value: 4.2 nM @ 4 mM ATP

Potency Assay: In vitro Kinase assay

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

Target aliases:

Macrophage colony-stimulating factor 1 receptor, F ...

DOI Reference: 10.1158/1535-7163.MCT-21-0361

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: KIT

Potency end-point : IC50 1600 nM

Potency assay (off target): Vimseltinib was profiled versus a total of approximately 300 human kinases at 10 mM ATP. Kinases inhibited within 1,000-fold of CSF1R were further tested at cellular levels of ATP (1–4 mmol/L).

Probe Selectivity in Vitro:

Vimseltinib was >100-fold selective for CSF1R versus all kinases tested and >1,000-fold selective for 294 kinases in this panel. Vimseltinib was >500-fold selective versus FLT3, KIT, PDGFRA, and PDGFRB.

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