Trametinib 10μM R02 exp83
Mechanism of Action
Inhibits MEK1 and MEK2, reversible allosteric mechanism, used in combination with BRAF V600E inhibitors
- Class / Subclass 1: Signal Transduction / Kinase Inhibitor
Technical Notes
Compound References
- PubChem Name: Trametinib
- Synonyms: GSK1120212; JTP-74057
- CAS #: 871700-17-3
- PubChem CID: 11707110
- IUPAC: N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide
- INCHI Name: 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)
- INCHI Key: LIRYPHYGHXZJBZ-UHFFFAOYSA-N
- Molecular Weight: 615.4
- Canonical SMILES: CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5
- Isomeric SMILES: N/A
- Molecular Formula: C26H23FIN5O4
Compound Supplier
- Supplier Name: Selleck Chemicals
- Catalog #: S2673
- Lot #: S267306
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C26H23FIN5O4 616.08515; found 616.08594
Dose Response Curve
- Platform ID: GSK1120212
- Min: -14.6969; Max: 3.8984
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | N/A |
| IC30 | N/A |
| IC40 | N/A |
| IC50 | N/A |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 02
- Dose: 10µM
- Days of incubation: 8
- Doublings: 6.0
- Numbers of reads: 12205762
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 5/2 | Scores |