Recently, Vorasidenib was approved as the first brain-penetrant dual inhibitor of mIDH1/2 for glioma treatment. The CF3 group is pivotal to this advancement, as its unique electronic properties enhance the molecule’s efficacy and selectivity. This modification not only enables the drug to penetrate the brain but also increases its potency in both enzyme and cell assays. Interestingly, the other two stereoisomers of Vorasidenib also showed nanomolar potency in the heterodimer mIDH1 enzymatic assay, though they exhibited slightly lower potency in cell assays. At Abovchem, a division of BirdoTech, we have developed the chemistry to produce these two essential chiral amines featuring the CF3 group. Please contact us if you are interested.