英文名稱 | Vorasidenib | AG-881 |
---|---|
中文名稱 | 6-(6-氯-2-吡啶基)-N2,N4-雙[(1R)-2,2,2-三氟-1-甲基乙基]-1,3,5-三嗪-2,4-二胺 |
CAS號(hào) | 1644545-52-7 |
分子式 | C14H13ClF6N6 |
分子量 | 414.74 |
外觀 | White to off-white |
英文名稱 | Vorasidenib | AG-881 |
---|---|
中文名稱 | 6-(6-氯-2-吡啶基)-N2,N4-雙[(1R)-2,2,2-三氟-1-甲基乙基]-1,3,5-三嗪-2,4-二胺 |
CAS號(hào) | 1644545-52-7 |
分子式 | C14H13ClF6N6 |
分子量 | 414.74 |
外觀 | White to off-white |
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
Targeting isocitrate dehydrogenase (IDH) in cancer.
PMID: 27355333
PMID: 31325170 DOI: 10.1002/bmc.4658
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective.
PMID: 29847930 DOI: 10.1021/acs.jmedchem.8b00159
Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): an Update and Perspective[J].
PMID: 29847930 DOI: 10.1021/acs.jmedchem.8b00159