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编 号：F748421
分子式：C30H44N4O8S
分子量：620.76
分子式：C30H44N4O8S
分子量：620.76
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CAS No: 2028300-31-2
产品详情
生物活性：
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M.
体内研究：
20S Proteasome-IN-2 (compoun 11m) is (i.v.; 5 mg/kg; single injection) rapidly cleared from the plasma with an average terminal plasma half-life of 14 min, thus it exhibits extensive tissue permeability and low clearance rate (CL) of 2.0 L/h/k, and is largely eliminated extrahepatically.20S Proteasome-IN-2 (compoun 11m) (i.v.; 10 mg/kg; twice one week; 4 weeks) shows antitumor efficacy combat solid tumors.Pharmacokinetic parameters of 20S Proteasome-IN-2 (compoun 11m)AdministrationsCmax (μg/L)AUC0-t (μg/L?h)T1/2 (min)MRT (min)CL (L/h/kg)Vss (L/kg)
iv, 5 mg/kg200768013.8320.202.00.66
Animal Model:HCT-116 cell xenograft nude mice model
Dosage:10 mg/kg
Administration:Intravenous injection; twice weekly for consecutive four weeks
Result:Inhibited tumor growth in vivo and was well tolerated.
体外研究：
20S Proteasome-IN-2 (compoun 11m) inhibits 20S proteasome by forming no irreversible covalent modification on it.20S Proteasome-IN-2 (compoun 11m) (1.56, 3.13, 6.25, 12.5, and 25 μM) shows high binding affinity with purified human 20S proteasome, the equilibrium dissociation constants is 4.8 μM.20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) inhibits tumor cells in a low concerntration with IC50 values of 0.88, 0.77, 0.67, 0.73, 1.3, 0.57, and 0.28 μM for A375, BGC-823, Hela, HT-29, A549, PCM1E8, HCT-116, resepectively.20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) arrests the cell cycle at G2/M.
20S Proteasome-IN-2 is a human 20S proteasome inhibitor. 20S Proteasome-IN-2 shows high selectivity to its β5 subunit with the IC50 of 0.18 μM. 20S Proteasome-IN-2 displays anti-proliferative effect in vitro and in vivo, and arrests cell cycle at G2/M.
体内研究：
20S Proteasome-IN-2 (compoun 11m) is (i.v.; 5 mg/kg; single injection) rapidly cleared from the plasma with an average terminal plasma half-life of 14 min, thus it exhibits extensive tissue permeability and low clearance rate (CL) of 2.0 L/h/k, and is largely eliminated extrahepatically.20S Proteasome-IN-2 (compoun 11m) (i.v.; 10 mg/kg; twice one week; 4 weeks) shows antitumor efficacy combat solid tumors.Pharmacokinetic parameters of 20S Proteasome-IN-2 (compoun 11m)AdministrationsCmax (μg/L)AUC0-t (μg/L?h)T1/2 (min)MRT (min)CL (L/h/kg)Vss (L/kg)
iv, 5 mg/kg200768013.8320.202.00.66
Animal Model:HCT-116 cell xenograft nude mice model
Dosage:10 mg/kg
Administration:Intravenous injection; twice weekly for consecutive four weeks
Result:Inhibited tumor growth in vivo and was well tolerated.
体外研究：
20S Proteasome-IN-2 (compoun 11m) inhibits 20S proteasome by forming no irreversible covalent modification on it.20S Proteasome-IN-2 (compoun 11m) (1.56, 3.13, 6.25, 12.5, and 25 μM) shows high binding affinity with purified human 20S proteasome, the equilibrium dissociation constants is 4.8 μM.20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) inhibits tumor cells in a low concerntration with IC50 values of 0.88, 0.77, 0.67, 0.73, 1.3, 0.57, and 0.28 μM for A375, BGC-823, Hela, HT-29, A549, PCM1E8, HCT-116, resepectively.20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) arrests the cell cycle at G2/M.
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