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MEK&P38 MAPK

Refametinib (RDEA119) (923032-37-5)

Refametinib (RDEA119, BAY 86-9766), is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity (IC50=19 nM MEK1; IC50=47 nM MEK2).

Not Intended for Therapeutic Use. For research use only.

CAS: 923032-37-5 Category

Refametinib (RDEA119) (923032-37-5) 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.

Refametinib (RDEA119) (923032-37-5) Specifications:

Product Name Refametinib
Synonym RDEA119; RDEA-119; RDEA 119; BAY 869766; BAY-69766; BAY869766; BAY 86 9766; BAY 86-9766; BAY86-9766; BAY 869766
Chemical Name (S)-N-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide
Drug Class N/A
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 923032-37-5
Molecular Formula C19H20F3IN2O5S
Molecular Weight 572.34
Monoisotopic Mass
572.009 g/mol

 

MDL number  
InChIKey RDSACQWTXKSHJT-NSHDSACASA-N
InChi Code InChI=1S/C19H20F3IN2O5S/c1-30-15-7-13(21)16(22)18(24-14-3-2-10(23)6-12(14)20)17(15)25-31(28,29)19(4-5-19)8-11(27)9-26/h2-3,6-7,11,24-27H,4-5,8-9H2,1H3/t11-/m0/s1
SMILES O=S(C1(C[[email protected]](O)CO)CC1)(NC2=C(OC)C=C(F)C(F)=C2NC3=CC=C(I)C=C3F)=O
Form solid powder
Color White
Solubility  Soluble in DMSO, not soluble in water.
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2. Potent MEK inhibitor.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Wylie-Sears J, Levine RA, Bischoff J. Losartan inhibits endothelial-to-mesenchymal transformation in mitral valve endothelial cells by blocking transforming growth factor-β-induced phosphorylation of ERK. Biochem Biophys Res Commun. 2014 Mar 12. pii: S0006-291X(14)00445-8. doi: 10.1016/j.bbrc.2014.03.014. [Epub ahead of print] PubMed PMID: 24632204.
  • 2: Weekes CD, Von Hoff DD, Adjei AA, Leffingwell DP, Eckhardt SG, Gore L, Lewis KD, Weiss GJ, Ramanathan RK, Dy GK, Ma WW, Sheedy B, Iverson C, Miner JN, Shen Z, Yeh LT, Dubowy RL, Jeffers M, Rajagopalan P, Clendeninn NJ. Multicenter phase I trial of the mitogen-activated protein kinase 1/2 inhibitor BAY 86-9766 in patients with advanced cancer. Clin Cancer Res. 2013 Mar 1;19(5):1232-43. doi: 10.1158/1078-0432.CCR-12-3529. Epub 2013 Feb 22. PubMed PMID: 23434733.
  • 3: Gorges TM, Schiller J, Schmitz A, Schuetzmann D, Schatz C, Zollner TM, Krahn T, von Ahsen O. Cancer therapy monitoring in xenografts by quantitative analysis of circulating tumor DNA. Biomarkers. 2012 Sep;17(6):498-506. doi: 10.3109/1354750X.2012.689133. Epub 2012 May 23. PubMed PMID: 22616911.
  • 4: Liu Z, Xing M. Induction of sodium/iodide symporter (NIS) expression and radioiodine uptake in non-thyroid cancer cells. PLoS One. 2012;7(2):e31729. doi: 10.1371/journal.pone.0031729. Epub 2012 Feb 16. PubMed PMID: 22359623; PubMed Central PMCID: PMC3281006.
  • 5: Holm TM, Habashi JP, Doyle JJ, Bedja D, Chen Y, van Erp C, Lindsay ME, Kim D, Schoenhoff F, Cohn RD, Loeys BL, Thomas CJ, Patnaik S, Marugan JJ, Judge DP, Dietz HC. Noncanonical TGFβ signaling contributes to aortic aneurysm progression in Marfan syndrome mice. Science. 2011 Apr 15;332(6027):358-61. doi: 10.1126/science.1192149. PubMed PMID: 21493862; PubMed Central PMCID: PMC3111087.

1 review for Refametinib (RDEA119) (923032-37-5)

  1. Cofttek

    Never had such good experience before,The Refametinib (RDEA119) (923032-37-5) is high purity,also customer service is pretty nice !gotta try!!

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