Trametinib (GSK1120212)

Trametinib (GSK1120212)

Author: ApexBio

spu:

A3018

CAS:

871700-17-3

purity:

0.9814

shortsummary:

MEK1 and MEK2 inhibitor, potent and selective

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Synonyms:

Trametinib, GSK-1120212, GSK1120212, Mekinist, JTP74057, JTP-74057

trichostatin a Purity

Formula:

C26H23FIN5O4

M.Wt:

615.39

Chemical Name:

N-[3-[3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxopyrido[4,3-d]pyrimidin-1-yl]phenyl]acetamide

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

Solubility:

insoluble in H2O; insoluble in EtOH; ≥15.38 mg/mL in DMSO

Storage:

Store at -20°C

Physical Appearance:

A solid

DeliveryTime:

In stock

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ShippingType:

Blue ice

description:

Trametinib (also known as GSK1120212 or JTP 74057), originally identified as a p15 inductive compound, is a novel and potent allosteric inhibitor of MEK kinase, which exhibits ATP non-competitive inhibition against MEK1 and MEK2 kinase. It has demonstrated broad antitumor activities in a variety of tumor xgenograft models, including HT-29 and COLO205 colorectal tumor cell lines. Trametinib induces expression of p15 and p27, reduces cyclin D1 levels, and causes dephosphorylation of RB protein and G1-phase arrest with a reduction of TS expression in HT-29 cells. It also effectively inhibits p-ERK 1/2 resulting in cell growth inhibition in tumor cell lines harboring B-RAF mutant.

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