For research use only. Not for therapeutic Use.
BI-847325（Cat No.:I004222）is a dual inhibitor targeting both MEK and Aurora kinases, key regulators in cell division and the MAPK signaling pathway. This compound has shown promise in cancer research, particularly in targeting tumors with mutations in the RAS/RAF/MEK pathway. By simultaneously inhibiting MEK and Aurora kinases, BI-847325 disrupts cell cycle progression and induces apoptosis in cancer cells, making it a potential therapeutic candidate for resistant tumors. Its dual-action mechanism provides a novel approach for overcoming drug resistance in certain types of cancer, such as melanoma and colorectal cancer.
| Catalog Number | I004222 |
| CAS Number | 1207293-36-4 |
| Synonyms | BI-847325; BI 847325; BI847325.;(Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide |
| Molecular Formula | C₂₉H₂₈N₄O₂ |
| 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 |
| Reference | </br>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 </br>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 </br>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 |
