| Identification | Back Directory | [Name]
Heptanamide, 7-[3-[[6-amino-4-(2-furanyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenoxy]-N-hydroxy- | [CAS]
2767560-94-9 | [Synonyms]
A2AAR/HDAC-IN-2
Heptanamide, 7-[3-[[6-amino-4-(2-furanyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]phenoxy]-N-hydroxy- | [Molecular Formula]
C23H26N6O4 | [MOL File]
2767560-94-9.mol | [Molecular Weight]
450.49 |
| Hazard Information | Back Directory | [Uses]
A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor[1]. | [IC 50]
HDAC1: 18.5 nM (IC50); HDAC2: 16.0 nM (IC50); HDAC3: 13.6 nM (IC50); HDAC6: 2.1 nM (IC50); HDAC8: 1408.9 nM (IC50); A1AR: 105.6 nM (Ki); A2AAR: 10.3 nM (Ki); A2BAR: 513.0 nM (Ki); A3AR: ＞10 μM (IC50) | [References]
[1] Zhang J, et al. Dual-acting antitumor agents targeting the A2A adenosine receptor and histone deacetylases: Design and synthesis of 4-(furan-2-yl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives. Eur J Med Chem. 2022 Jun 5;236:114326. DOI:10.1016/j.ejmech.2022.114326 |
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