Chemical Probes logo
Capmatinib | Capmatinib : ATP competitive inhibitor of MET
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MET
  • IC50:0.13 nM
  • Kd:0.31 nM
  • IC50:0.3-1.1 nM
ATP competitive
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
inactive against RONβ; profiled against a panel of 57 human kinases representing a structurally d ...

Potency
Cellular
In Vitro

MET

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/1078-0432.CCR-11-1157

In Vivo Validations

Mouse
Dose: 0.03, 0.1, 0.3, 1, 3, or 10 mg/kg, Reviewer suggested: 3, 10, and 30 mg/kg BID
Route of delivery: Oral

DOI Reference: 10.1158/1078-0432.CCR-18-2814

Orthogonal Probes def

MK-8033
AMG-337
SULFUR, PRECIPITATED

Chemical Information

Molecular Formula C23H17FN6O
SMILEs CNC(=O)c1ccc(-c2cnc3ncc(Cc4ccc5ncccc5c4)n3n2)cc1F
InChI InChI=1S/C23H17FN6O/c1-25-22(31)18-6-5-16(11-19(18)24)21-13-28-23-27-12-17(30(23)29-21)10-14-4-7-20-15(9-14)3-2-8-26-20/h2-9,11-13H,10H2,1H3,(H,25,31)
Molecular weight 412.14 Da
AlogP 0.0
HBond acceptors 7
HBond donors 1
Atoms 48

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 3 Dec 2020 )
Cellular Use Rating
In Model Organisms
INCB28060 / capmatinib is a potent c-MET inhibitor, which shows excellent selectivity in a broad panel of 442 kinases. Sub nM-activity is observed at wt and mutant (M1250T, Y1235D) c-Met, with most-active...
by SERP
(on 14 Dec 2020 )
Cellular Use Rating
In Model Organisms
Capmatinib (INC280) is an exceptionally potent and kinome-selective inhibitor of c-Met. The on-target potency is sub-nM. Using both a limited panel of 57 kinases and the larger 442 kinases KINOMEscan...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria