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AGI-24512

CAS No. : 2201066-53-5

MCE 國際站：AGI-24512

產(chǎn)品活性：AGI-24512 是一種蛋氨酸腺苷轉(zhuǎn)移酶 2α (MAT2A) 抑制劑，IC₅₀ 為 8 nM。AGI-24512 觸發(fā) DNA 損傷反應(yīng)。AGI-24512 可阻斷 MTAP 缺失的癌細(xì)胞體外增殖。AGI-24512可用于抗癌研究。

研究領(lǐng)域：Epigenetics  |  Metabolic Enzyme/Protease

作用靶點(diǎn)：Methionine Adenosyltransferase (MAT)

In Vitro: AGI-24512 (0-1 μM; 96 hours) blocks proliferation of MTAP (methylthioadenosine phosphorylase)-deleted HCT116 cancer cells with an IC₅₀ of 100 nM.
?AGI-24512 significantly increases in γH2AX-positive cells in MTAP^-/- HCT116 cells.
?AGI-24512 inhibits PRMT5-mediated SDMA marks with an IC₅₀ of 95 nM in MTAP^-/- cells.
?AGI-24512 leads to a dose-dependent decrease in SAM (S-adenosylmethionine) levels in the HCT116 MTAP-null cell, with an IC₅₀ of 100 nM.

In Vivo: AGI-24512 shows poor oral absorption and a short half-life in rats.

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