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).
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CX-5461 dihydrochloride
CAS number:unknown molecular formula:C27H29Cl2N7O2S
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| Chinese alias | CX-5461 二盐酸盐 | ||
| English alias | - | ||
| CAS number | unknown | molecular formula | C27H29Cl2N7O2S |
| molecular weight | 586.54 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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