Vorasidenib (Synonyms: AG-881) |
| Catalog No.GC19380 |
보라시데닙(AG-881)은 경구로 사용 가능한 뇌 침투 2세대 이중 돌연변이 이소시트레이트 탈수소효소 1 및 2(mIDH1/2) 억제제입니다. 보라시데닙(AG-881)은 (D)-2-하이드록시글루타레이트(D-2-HG)의 나노몰 억제를 나타내며 IDH1 R132C, IDH1 R132G, IDH1 R132H 및 IDH1 R1342S 및 7~1에 대해 IC50 범위가 0.04~22 nM입니다. IDH2 R140Q에 대한 nM 및 IDH2 R172K에 대한 130nM.
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Cas No.: 1644545-52-7
Sample solution is provided at 25 µL, 10mM.
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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[1][2].
Vorasidenib has strong antiproliferative activity against human glioblastoma U-87 MG pLVX-IDH2 R140Q-neo, fibrosarcoma HT-1080 and neurosphere TS603 cells, all with IC50s of less than 50 nM[2].
References:
[1]. Fujii T, et al. Targeting isocitrate dehydrogenase (IDH) in cancer. Discov Med. 2016 May;21(117):373-80.
[2]. Ma T, et al. Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective. J Med Chem. 2018 Oct 25;61(20):8981-9003.
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