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GSK 1120212
- Trametinib - JTP 74057
- Soluble in DMSO
- MF: C26H23FIN5O4
- MW: 615.39
Description
GSK 1120212 is a highly potent and selective MEK1/MEK2 inhibitor with IC50 values of 0.7 nM for MEK1 and 0.9 nM for MEK2.
MEK1/2 are central kinases in the RAS-RAF-MEK-ERK pathway and regulate proliferation and survival downstream of oncogenic RAF and RAS. GSK 1120212 (Trametinib) is a key reference compound for MAPK pathway inhibition.
Key Features
- Potent MEK1 and MEK2 inhibitor
- IC50: 0.7 nM for MEK1 and 0.9 nM for MEK2
- Highly selective MAPK pathway inhibitor
- Clinically validated ERK pathway pharmacology
Applications
- RAS-RAF-MEK-ERK signaling studies
- Cancer cell proliferation assays
- MAPK pathway resistance research
- Kinase inhibitor pharmacology
More Information
| Parent CAS No. | 871700-17-3 |
|---|---|
| Chemical Name | N-(3-(3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl)phenyl)acetamide |
| SMILES | C1C(N2C(=O)N(C3CC3)C(=O)C3=C(NC4C(F)=CC(I)=CC=4)N(C)C(=O)C(C)=C23)=CC(NC(=O)C)=CC=1 |
| MFCD | N.A. |
| 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) |
| InChiKey | LIRYPHYGHXZJBZ-UHFFFAOYSA-N |
| CID | 11707110 |
| Short Description | MEK inhibitor |
References
- AG Gilmartin et al. GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin. Cancer Res. 2011, 17(5), 989-1000.
- T Yamaguchi et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int J Oncol. 2011, 39(1), 23-31.
- H Abe et al. Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate). ACS Med. Chem. Lett., 2011, 2(4), 320–324.
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