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GSK 1120212  - JTP 74057 - Trametinib

CAS 871700-17-3

C26H23FIN5O4  MW 615.39 

Purity: 99%

Soluble in DMSO

 

 

 

 

 

Ordering Information:

 

Cat. No. Axon 1761   Prime Source

 

Qty1: 5 mg (research sample) / €125  $163

Promotion: 2 x 5 mg @ €180  $234

Qty2: 25 mg (research sample) / €425  $553

Promotion: 2 x 25 mg @ €640  $832

Qty3: on request

 

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Biological Activity:

 

Highly potent and selective MEK inhibitor, with IC50 values to be 0.7 and 0.9 nM for MEK1 and MEK2 respectively and with long circulating half-life.

 

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. [online]


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. [online]

 

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. [online]

 

 

Chemical Name: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodophenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide

 

GSK 1120212 | MEK inhibitor | Axon Medchem | Axon 1761 | GSK1120212

Axon Ligands TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.

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Axon Ligands In This Field:

 

AZD 6244 | MEK inhibitor

GSK 1120212 | MEK inhibitor

PD 98059 | MEK inhibitor

PD 184352 | MEK inhibitor

PD 0325901 | MEK inhibitor

SL 327 | MEK inhibitor

 

BIRB 796 | p38 MAPK inhibitor

PD 169316 | p38 MAPK inhibitor

SB 203580 | p38 MAPK inhibitor

SB 202190 | p38 MAPK inhibitor

SCIO 469 | p38 MAPK inhibitor

SD 169 | p38α MAPK inhibitor

 

FR 180204 | ERK inhibitor

XMD8-92 | BMK1 inhibitor

 

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