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| Cas No.: | 1256094-72-0 |
| Chemical Name: | 2,2'-(5,5'-((oxybis(ethane-2,1-diyl))bis(oxy))bis(pyridine-5,2-diyl))bis(5-(trifluoromethoxy)-1H-benzo[d]imidazole) |
| Synonyms: | AI 1049,AI1049 |
| SMILES: | C(C1=NC=C(OCCOCCOC2=CC=C(C3=NC4=CC(OC(F)(F)F)=CC=C4N3)N=C2)C=C1)1=NC2=CC(OC(F)(F)F)=CC=C2N1 |
| Formula: | C30H22F6N6O5 |
| M.Wt: | 660.52 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | AI-10-49 is a protein-protein interaction inhibitor that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1 with a FRET IC50 of 0.26 uM.AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics,and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers. |