RDEA119 (REFAMETINIB)

Background Information:

RDEA119 is a potent, highly selective and orally-bioavailable small
molecule allosteric MEK inhibitor with IC50 at low nM, currently in
clinical trials.

Reference:

1. Maderna, Andreas; Vernier, Jean-Michel; Barawkar, Dinesh; El,
Abdellaoui Hassan; Hong, Zhi. Preparation of N-(arylamino)-sulfonamide
inhibitors of MEK. Braz. Pedido PI (2009), 121pp. CODEN: BPXXDX BR
2008000989 A2 20090922 CAN 152:262363 AN 2010:280107.
2. Quart, Barry D.; Rowlings, Colin Edward. Preparation of
phenylaminophenylsulfonamides for treatment of cancer and inflammatory
disease. PCT Int. Appl. (2009), 234 pp. CODEN: PIXXD2 WO 2009129246 A2
20091022 CAN 151:448059 AN 2009:1294093.
3: Iverson, Cory; Larson, Gary; Lai, Chon; Yeh, Li-Tain; Dadson,
Claudia; Weingarten, Paul; Appleby, Todd; Vo, Todd; Maderna, Andreas;
Vernier, Jean-Michel; Hamatake, Robert; Miner, Jeffrey N.; Quart, Barry.
RDEA119/BAY 869766: A Potent, Selective, Allosteric Inhibitor of MEK1/2
for the Treatment of Cancer. Cancer Research (2009), 69(17), 6839-6847.

APIM050233: RDEA119 (REFAMETINIB)

CAS No.: 923032-37-5.
Molecular Formula: C₁₉H₂₀F₃IN₂O₅S.
Molecular Weight: 572.3.
Purity: >99% chem and optical purity (HPLC and chiral HPLC).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.