Refametinib

• CAT Number: I005488
• CAS Number: 923032-37-5
• Molecular Formula: C₁₉H₂₀F₃IN₂O₅S
• Molecular Weight: 572.34
• Purity: ≥95%
• Target: MEK1/2
• Solubility: DMSO：≥ 31 mg/mL
• Storage: Store at -20℃
• IC50: 19 nM (MEK1); 47 nM (MEK2)
• IUPAC Name: N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide
• InChI: 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
• InChIKey: RDSACQWTXKSHJT-NSHDSACASA-N
• SMILES: COC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)CC(CO)O)NC3=C(C=C(C=C3)I)F)F)F

Refametinib (Cat.No:I005488) is a potent and selective MEK inhibitor. MEK, a mitogen-activated protein kinase (MAPK) kinase, plays a crucial role in cell growth and proliferation pathways. Refametinib has shown promise in preclinical and clinical studies as a potential treatment for various cancers, including melanoma and other solid tumors.

Reference

1:Phase I/II Study of Refametinib (BAY 86-9766) in Combination with Gemcitabine in Advanced Pancreatic cancer. Van Laethem JL, Riess H, Jassem J, Haas M, Martens UM, Weekes C, Peeters M, Ross P, Bridgewater J, Melichar B, Cascinu S, Saramak P, Michl P, Van Brummelen D, Zaniboni A, Schmiegel W, Dueland S, Giurescu M, Garosi VL, Roth K, Schulz A, Seidel H, Rajagopalan P, Teufel M, Childs BH.Target Oncol. 2017 Feb;12(1):97-109. doi: 10.1007/s11523-016-0469-y. PMID: 27975152 2:A Phase I Study of the Safety, Pharmacokinetics, and Pharmacodynamics of Combination Therapy with Refametinib plus Sorafenib in Patients with Advanced Cancer. Adjei AA, Richards DA, El-Khoueiry A, Braiteh F, Becerra CH, Stephenson JJ Jr, Hezel AF, Sherman M, Garbo L, Leffingwell DP, Iverson C, Miner JN, Shen Z, Yeh LT, Gunawan S, Wilson DM, Manhard KJ, Rajagopalan P, Krissel H, Clendeninn NJ.Clin Cancer Res. 2016 May 15;22(10):2368-76. doi: 10.1158/1078-0432.CCR-15-1681. Epub 2015 Dec 7. PMID: 26644411 Free Article3:A phase II study of the efficacy and safety of the combination therapy of the MEK inhibitor refametinib (BAY 86-9766) plus sorafenib for Asian patients with unresectable hepatocellular carcinoma. Lim HY, Heo J, Choi HJ, Lin CY, Yoon JH, Hsu C, Rau KM, Poon RT, Yeo W, Park JW, Tay MH, Hsieh WS, Kappeler C, Rajagopalan P, Krissel H, Jeffers M, Yen CJ, Tak WY.Clin Cancer Res. 2014 Dec 1;20(23):5976-85. doi: 10.1158/1078-0432.CCR-13-3445. Epub 2014 Oct 7. PMID: 25294897 Free Article4:Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma. Schmieder R, Puehler F, Neuhaus R, Kissel M, Adjei AA, Miner JN, Mumberg D, Ziegelbauer K, Scholz A.Neoplasia. 2013 Oct;15(10):1161-71. PMID: 24204195 Free PMC Article