BI-847325

• CAT Number: I004222
• CAS Number: 1207293-36-4
• Molecular Formula: C₂₉H₂₈N₄O₂
• Molecular Weight: 464.57
• Purity: ≥95%
• Target: MEK1/2
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20°C
• IUPAC Name: 3-[3-[N-[4-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indol-6-yl]-N-ethylprop-2-ynamide
• InChI: InChI=1S/C29H28N4O2/c1-4-30-26(34)17-13-20-12-16-24-25(18-20)32-29(35)27(24)28(22-8-6-5-7-9-22)31-23-14-10-21(11-15-23)19-33(2)3/h5-12,14-16,18,32,35H,4,19H2,1-3H3,(H,30,34)
• InChIKey: OCUQMWSIGPQEMX-UHFFFAOYSA-N
• SMILES: CCNC(=O)C#CC1=CC2=C(C=C1)C(=C(N2)O)C(=NC3=CC=C(C=C3)CN(C)C)C4=CC=CC=C4

BI-847325（Cat No.:I004222） is an orally active and selective inhibitor that targets both MEK (Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase) and Aurora kinase. MEK is involved in cell growth and proliferation pathways, while Aurora kinase regulates cell division. By inhibiting both targets, BI-847325 can disrupt cellular signaling and inhibit tumor growth. Its selectivity allows for more specific targeting of these pathways.

Reference

1:Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases. Sini P, Gürtler U, Zahn SK, Baumann C, Rudolph D, Baumgartinger R, Strauss E, Haslinger C, Tontsch-Grunt U, Waizenegger IC, Solca F, Bader G, Zoephel A, Treu M, Reiser U, Garin-Chesa P, Boehmelt G, Kraut N, Quant J, Adolf GR.Mol Cancer Ther. 2016 Oct;15(10):2388-2398. Epub 2016 Aug 5. PMID: 27496137 2:A phase I study of two dosing schedules of oral BI 847325 in patients with advanced solid tumors. Schöffski P, Aftimos P, Dumez H, Deleporte A, De Block K, Costermans J, Billiet M, Meeus MA, Lee C, Schnell D, Goeldner RG, Awada A.Cancer Chemother Pharmacol. 2016 Jan;77(1):99-108. doi: 10.1007/s00280-015-2914-5. Epub 2015 Dec 9. PMID: 26650227 3:The Novel ATP-Competitive MEK/Aurora Kinase Inhibitor BI-847325 Overcomes Acquired BRAF Inhibitor Resistance through Suppression of Mcl-1 and MEK Expression. Phadke MS, Sini P, Smalley KS.Mol Cancer Ther. 2015 Jun;14(6):1354-64. doi: 10.1158/1535-7163.MCT-14-0832. Epub 2015 Apr 14. PMID: 25873592 Free PMC Article