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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis , with IC 50 s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II ( IC 50 ≥25 μM).
Appearance:Solid
IC50& Target:IC50: 54 nM (rRNA synthesis, MIA PaCa-2 cells), 113 nM (rRNA synthesis, A375 cells), 142 nM (rRNA synthesis, HCT-116 cells)
In Vitro:CX-5461 is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC 50 s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC 50 , ≥25 μM). CX-5461 has modest inhibiti
In Vivo:CX-5461 displays antitumor activity against human solid tumors in murine xenograft models. CX-5461 (50mg/kg, p.o.) shows significant MIA PaCa-2 growth inhibition with TGI equal to 69% on day 31 and 79% TGI on A375 on day 32. CX-5461 (50mg/kg, p.o.)
Biological Activity:CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis , with IC 50 s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II ( IC 50 ≥25 μM).