AI-10-49

CAS NO.:1256094-72-0

Molecular Formula:C₃₀H₂₂F₆N₆O₅

Molecular Weight:660.52

Purity: > 98%

Solubility (R.T.: 25℃): DMSO

Stability: - 20℃ 2 years

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. IC50 value: 0.26 uM [1] Target: CBFβ-SMMHC/RUNX1 interaction inhibitor 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. 

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