| Identification | Back Directory | [Name]
AGI-24512 | [CAS]
2201066-53-5 | [Synonyms]
AGI-24512
Pyrazolo[1,5-a]pyrimidin-7(4H)-one, 6-(4-hydroxyphenyl)-5-methyl-2-phenyl-3-(1-piperidinyl)- | [Molecular Formula]
C24H24N4O2 | [MOL File]
2201066-53-5.mol | [Molecular Weight]
400.47 |
| Chemical Properties | Back Directory | [Boiling point ]
639.3±65.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 125 mg/mL (312.13 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
9.47±0.30(Predicted) | [color ]
White to gray |
| Hazard Information | Back Directory | [Description]
AGI-24512 is a MATA2 inhibitor that are useful as therapeutic agents for treating malignancies. AGI-24512 showed in vivo activity in MTAP null tumors. | [Uses]
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer[1]. | [in vivo]
AGI-24512 shows poor oral absorption and a short half-life in rats[2]. | [storage]
Store at -20°C | [References]
[1] Kalev P, et al. MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. DOI:10.1016/j.ccell.2020.12.010
[2] Konteatis Z, et al. Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion. J Med Chem. 2021 Apr 22;64(8):4430-4449. DOI:10.1021/acs.jmedchem.0c01895 |
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