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Showing 1 - 10 of 20 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 (2015)
First approved in 2015

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cobimetinib is an orally active, potent and highly selective small molecule inhibiting mitogen-activated protein kinase kinase 1 (MAP2K1 or MEK1), and central components of the RAS/RAF/MEK/ERK signal transduction pathway. It has been approved in Swit...
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)



RO4987655 is a highly selective non-competitive small molecule inhibitor of MEK. RO4987655 has a strong anti-proliferation efficacy in various tumor cells including COLO205, HT29, QG56, MIA and C32 with IC50 values of 0.86nM, 1.7nM, 9.5nM, 3.3nM and ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ABSOLUTE)



TAK-733 had been developed by Millennium Pharmaceuticals (subsidiary of Takeda) for the treatment of adult patients with advanced non-hematological malignancies. In 2015, Takeda discontinued this studies. TAK-733 is an inhibitor of MEK that exhibits ...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)



DC-0623 is an orally active, selective and ATP-uncompetitive MEK inhibitor with potential antineoplastic activity. GDC-0623 specifically inhibits mitogen-activated protein kinase kinase (MEK or MAP/ERK kinase), resulting in inhibition of growth facto...
Status:
Investigational

Class (Stereo):
CHEMICAL (ACHIRAL)


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...

Showing 1 - 10 of 20 results