产品
编 号：F755913
分子式：C53H61ClN8O5S
分子量：957.62
分子式：C53H61ClN8O5S
分子量：957.62
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CAS No: 2770108-93-3
产品详情
生物活性：
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
体内研究：
YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.Pharmacokinetic Parameters of YM458 in Female BALB/c mice.IP (80 mg/kg) PO (80 mg/kg)
t1/2 (h)3.814.16
Tmax (h)11
Cmax (ng/mL)27126.34383.6
AUC0-24 (ng/mL·h)273220.113509.1
CL (mL/min/kg)4.88
F (%)4.94
Animal Model:BALB/c nude mice (injected with A549 or AsPC-1)
Dosage:60 mg/kg
Administration:IP; every other day, for 38 days
Result:Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.
体外研究：
YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50 of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1.YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner.
YM458 is a potent EZH2 and BRD4 dual inhibitor with IC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest and apoptosis in solid cancer cells. YM458 can be used for researching anticancer.
体内研究：
YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.Pharmacokinetic Parameters of YM458 in Female BALB/c mice.IP (80 mg/kg) PO (80 mg/kg)
t1/2 (h)3.814.16
Tmax (h)11
Cmax (ng/mL)27126.34383.6
AUC0-24 (ng/mL·h)273220.113509.1
CL (mL/min/kg)4.88
F (%)4.94
Animal Model:BALB/c nude mice (injected with A549 or AsPC-1)
Dosage:60 mg/kg
Administration:IP; every other day, for 38 days
Result:Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells.
体外研究：
YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50 of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1.YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM.YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner.
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