CX-5461 dihydrochloride

CX-5461 二盐酸盐

CX-5461 dihydrochloride

C658617-5mg

5mg

≥98%

2-8°C储存,干燥

冰袋运输

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).

C27H29Cl2N7O2S

586.54 g/mol

[H]Cl.CC1=NC=C(CNC(C2=C3N(C4=NC(N5CCN(CCC5)C)=CC=C4C2=O)C6=C(S3)C=CC=C6)=O)N=C1.[H]Cl

H2O : 5 mg/mL (8.52 mM; ultrasonic and warming and heat to 80°C)