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CX-5461 dihydrochloride

CAS number:unknown    molecular formula:C27H29Cl2N7O2S

overview

compound introduction

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).

Specs

Chinese aliasCX-5461 二盐酸盐
English alias-
CAS numberunknownmolecular formulaC27H29Cl2N7O2S
molecular weight586.54 g/molExact mass≥98%
PSA-logp-

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