Brigatinib

Inhibitor of ALK

Structure

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Probe Brigatinib is in the process of SERP review.

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Information

Inhibitor

up to 500 nM

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Probe Availability:

In Vitro Validations

Uniprot ID: Q9UM73

Target Class: Kinase

Target SubClass: RTK

Potency: IC50

Potency Value: 0.6 nM WT; 0.6 nM C1156Y; 1.4 nM F1174L; 1.7 nM L1196M; 4.9 nM G1202R; 6.6 nM R1275Q

Potency Assay: Kinase Assay @ 10 uM ATP

PDB ID for probe-target interaction (3D structure): 6MX8

Structure-activity relationship: yes

Target aliases:

ALK tyrosine kinase receptor, ALK, ALK_HUMAN, Anap ...

DOI Reference: 10.1021/acs.jmedchem.6b00306

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

In vitro HotSpotSM kinase profiling of 289 kinases: ∼4% (11 out of 289) of the kinases were inhibited with IC50’s of <10 nM. No activity against c-Met or Ron @ 1 uM.

Potency in cells, off target : IC50 18 nM CD74-ROS1, 158 nM FLT3-ITD

Probe Selectivity in Cell:

IC50s (nM): >3,000 p-EGFR in EGF-stimulated H358 cells, 397 EGFR (L858R), 489 EGFR (L858R/T790M), 148 p-IGF-1R in IGF1-stimulated HepG2 cells, 9331 p-INSR in insulin-stimulated H-4-II-E cells.

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No SERP comments found for Brigatinib