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Showing 1 - 10 of 10 results

Status:
US Approved Rx (2025)
First approved in 2025

Class (Stereo):
CHEMICAL (ABSOLUTE)



PD-0325901 is an orally bioavailable inhibitor of mitogen-activated protein kinase kinases (MAPK/ERK kinases or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhib...
Status:
US Approved Rx (2020)
First approved in 2020

Class (Stereo):
CHEMICAL (ACHIRAL)



Selumetinib (AZD6244 or ARRY-142886) is a potent, selective, and ATP-uncompetitive inhibitor of Ras-Raf-mitogen-activated protein kinase kinase (MEK1/2). This inhibition can prevent ERK activation, disrupt downstream signal transduction, and inhibit ...
Status:
US Approved Rx (2018)
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Binimetinib (MEK162) is an oral small-molecule with potential antineoplastic activity. It is a selective mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, a key protein kinase in the RAS/RAF/MEK/ERK pathway, which regulates several key cel...
Status:
US Approved Rx (2023)
First approved in 2013

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Trametinib is a reversible and specific inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2 which are involved in a RAS/RAF/MEK/ERK signaling pathway and control cell growth, survival, and differentiation. By inhibiting MEK1 and MEK2 ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



Refametinib (RDEA-119, BAY- 869766) is a highly potent and selective inhibitor of mitogen-activated ERK kinase (MEK1/2) activity, Refametinib binds to an allosteric pocket adjacent to the ATP binding site, locking the enzyme in a catalytically inacti...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)



CI 1040 is an inhibitor of the mitogen-activated protein (MAP) kinase signal transduction pathway and has been shown to specifically inhibit MAP kinase kinase (MEK). CI 1040 was being developed by Parke-Davis (formerly a division of WarnerLambert, No...
Status:
Designated

Class (Stereo):
CHEMICAL (ACHIRAL)


U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. The inhibitory effects of U0126 on MEK and ERK activation have been confirmed repeatedly, and treatments with U0126 have been shown to inhibit proliferation and m...
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

BI-847325 is a novel, ATP-competitive, orally available inhibitor of Aurora kinases and MEK. In in vitro studies, BI-847325 inhibited the activity of Xenopus laevis Aurora Kinase B with an IC50 of 3 nM; with IC50 values for human Aurora kinase A and ...
Status:
US Approved Rx (2020)
First approved in 2020

Class (Stereo):
CHEMICAL (ACHIRAL)



Selumetinib (AZD6244 or ARRY-142886) is a potent, selective, and ATP-uncompetitive inhibitor of Ras-Raf-mitogen-activated protein kinase kinase (MEK1/2). This inhibition can prevent ERK activation, disrupt downstream signal transduction, and inhibit ...
Status:
US Approved Rx (2023)
First approved in 2013

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Trametinib is a reversible and specific inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2 which are involved in a RAS/RAF/MEK/ERK signaling pathway and control cell growth, survival, and differentiation. By inhibiting MEK1 and MEK2 ...