Chemical Probes logo
Trametinib | Trametinib : Allosteric inhibitor of MAP2K1, MAP2K2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAP2K1
  • IC 50:0.92 nM
  • IC50:9.8 nM ACHN; 0.57 nM HT-29
MAP2K2
  • IC 50:1.8 nM
  • IC50:0.57 nM
  • IC 50:9.8 nM
Allosteric
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
No inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. No relevant inhibition det ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Trametinib exhibited over 50-fold selectivity for cancer cells relative to normal tissues and hem ...

Potency
Cellular
In Vitro

MAP2K1

Mode of Action: Allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml200004g

MAP2K2

Mode of Action: Allosteric

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml200004g

In Vivo Validations

Mouse
Dose: 0.1-1 mg/Kg
Route of delivery: Oral

DOI Reference: 10.1021/ml200004g

Orthogonal Probes def

SELUMETINIB

Chemical Information

Molecular Formula C26H23FIN5O4
SMILEs CC(=O)Nc1cccc(-n2c(=O)n(C3CC3)c(=O)c3c(Nc4ccc(I)cc4F)n(C)c(=O)c(C)c32)c1
InChI InChI=1S/C26H23FIN5O4/c1-13-22-21(23(31(3)24(13)35)30-20-10-7-15(28)11-19(20)27)25(36)33(17-8-9-17)26(37)32(22)18-6-4-5-16(12-18)29-14(2)34/h4-7,10-12,17,30H,8-9H2,1-3H3,(H,29,34)
Molecular weight 615.08 Da
AlogP 3.94012
HBond acceptors 9
HBond donors 2
Atoms 60

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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

Expert Reviews

No SERP comments found for Trametinib

Probe Trametinib is in the process of SERP review.

Please continue to check back for new reviews and commentary.