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KI3719Refametinib5 mg$184

Chemical Characteristic

Product NameRefametinib
SynonymsRDEA119, BAY 86-9766
CAS No.923032-37-5
Molecular Weight 572.34
FormulaC19H20N2O5F3SI
Chemical Name(S)-N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
SmilesC1(CC1)(S(=O)(=O)Nc1c(c(c(cc1OC)F)F)Nc1c(cc(cc1)I)F)C[C@@H](CO)O
Chemical Structure

Biological activities

Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. Refametinib specifically inhibits mitogen-activated protein kinase kinase 1 (MAP2K1 or MAPK/ERK kinase 1), resulting in inhibition of growth factor-mediated cell signaling and tumor cell proliferation. MEK, a dual specificity threonine/tyrosine kinase, is a key component of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth; constitutive activation of this pathway has been implicated in many cancers [1]. In vitro, it can be used by 0.3 ?M in human Hep3B cells [2].

References

[1] Ramfidis VS, Psyrri A, Syrigos KN, et al. First line treatment for metastatic pancreatic adenocarcinoma: looking for the step forward. JOP. 2014,15(4):286-288.
[2] Schmieder R, Puehler F, Neuhaus R, et al. Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma. Neoplasia. 2013, 15(10):1161-1171.

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