For research use only. Not for therapeutic Use.
MI-463 is a potent menin-MLL inhibitor with IC50=15.3 nM and Kd=9.9 nM. MI-463 shows its profound effects in MLL leukemia cells and substantial survival benefit in mouse models of MLL leukemia. Pharmacologic inhibition of the menin-MLL interaction represents an effective treatment for MLL leukemias in vivo and provide advanced molecular scaffold for clinical lead identification. Chromosomal translocations affecting mixed lineage leukemia gene (MLL) result in acute leukemias resistant to therapy. The leukemogenic activity of MLL fusion proteins is dependent on their interaction with menin, providing basis for therapeutic intervention.
| Catalog Number | I007981 |
| CAS Number | 1628317-18-9 |
| Synonyms | MI-463; MI 463; MI463.;4-methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile |
| Molecular Formula | C24H23F3N6S |
| Purity | ≥95% |
| Target | Epigenetic Reader Domain |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IC50 | 15.3 nM |
| SMILES | CC1=C2C(NC(C#N)=C2)=CC=C1CN(CC3)CCC3NC4=C(C=C(CC(F)(F)F)S5)C5=NC=N4 |
| Reference | </br>1:Borkin D, He S, Miao H, Kempinska K, Pollock J, Chase J, Purohit T, Malik B, Zhao T, Wang J, Wen B, Zong H, Jones M, Danet-Desnoyers G, Guzman ML, Talpaz M, Bixby DL, Sun D, Hess JL, Muntean AG, Maillard I, Cierpicki T, Grembecka J. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell. 2015 Apr 13;27(4):589-602. doi: 10.1016/j.ccell.2015.02.016. Epub 2015 Mar 26. PubMed PMID: 25817203; PubMed Central PMCID: PMC4415852. |
