Name: Refametinib
CAS#: 923032-37-5
Chemical Formula: C19H20F3IN2O5S
Exact Mass: 572.00897
Molecular Weight: 572.34
Elemental Analysis: C, 39.87; H, 3.52; F, 9.96; I, 22.17; N, 4.89; O, 13.98; S, 5.60
EOS Med Chem produce Refametinib,RDEA-119,BAY 869766, 923032-37-5 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.
Refametinib,RDEA-119,BAY 869766, 923032-37-5 Intermediates, EOS Med Chem have 8; Refametinib,RDEA-119,BAY 869766, 923032-37-5 Impurity we have 10, all from GMP, FDA plant.
Now Refametinib,RDEA-119,BAY 869766, 923032-37-5 DMF document is preparing.
Until 2016, Aug, Refametinib,RDEA-119,BAY 869766, 923032-37-5 more than produced 25kg API, 120kg Intermediates
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Refametinib BAY-86-9766; AY-869766; RDEA-119; AR-119 923032-37-5
Refametinib Intermediates (S)-tert-butyldimethyl(oxiran-2-ylmethoxy)silane 123237-62-7
Refametinib Intermediates Butyl cyclopropanesulfonate 83635-12-5
Refametinib Intermediates (S)-butyl 1-(3-((tert-butyldimethylsilyl)oxy)-2-hydroxypropyl)cyclopropane-1-sulfonate 1335100-23-6
Refametinib Intermediates (S)-butyl 1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonate 1335100-30-5
Refametinib Intermediates (S)-butyl 1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonate 1335100-31-6
Refametinib Intermediates Sodium (S)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonate 1262760-34-8
Refametinib Intermediates (S)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonyl chloride 1262760-00-8
Refametinib Intermediates 2,3,5-trifluoro-N-(3-fluoro-4-iodophenyl)-6-nitroaniline 765962-71-8
Refametinib Intermediates 2,3-difluoro-N-(2-fluoro-4-iodophenyl)-5-methoxy-6-nitroaniline 923032-72-8
Refametinib Intermediates 5,6-difluoro-N1-(2-fluoro-4-iodophenyl)-3-methoxybenzene-1,2-diamine 923032-74-0
Refametinib Intermediates (S)-N-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-6-methoxyphenyl)-1-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)cyclopropane-1-sulfonamide 1262760-18-8
Description: Refametinib, also known as RDEA119, BAY 86-9766, is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity. MEK inhibitor RDEA119 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.
Synonym: RDEA119; RDEA-119; RDEA 119; BAY 869766; BAY-69766; BAY869766; BAY 86 9766; BAY 86-9766; BAY86-9766; BAY 869766
IUPAC/Chemical Name: (S)-N-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
SMILES Code: O=S(C1(C[C@H](O)CO)CC1)(NC2=C(OC)C=C(F)C(F)=C2NC3=CC=C(I)C=C3F)=O
BAY 86-9766, formerly known as RDEA119, is currently being developed by Ardea. BAY 86-9766 is a potent, non-ATP competitive, highly-selective inhibitor of MEK. According to Ardea Inc's website, preclinical and clinical data suggest that BAY 86-9766 has favorable properties, including once-daily, oral dosing, excellent selectivity and limited retention in the brain, which may result in a reduced risk of central nervous system (CNS) side effects at doses expected to be effective, a problem associated with other members of this class of compounds. In addition, BAY 86-9766 has been shown to suppress tumor cell growth in-vitro and in-vivo. Phase 1 data have demonstrated that BAY 86-9766 has a long half-life and favorable pharmacokinetic properties, allowing for once-daily oral dosing. Preclinical in vitro and in vivo oncology studies have demonstrated significant potential synergy across multiple tumor types when BAY 86-9766 is used in combination with other approved anti-cancer therapeutics, including sorafenib (Nexavar®; Bayer HealthCare, Onyx Pharmaceuticals). (source: http://www.ardeabio.com/development-pipeline/cancer.htm ).
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