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编 号：F500714
分子式：C28H26O8
分子量：490.5
分子式：C28H26O8
分子量：490.5
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CAS No: 886578-07-0
产品详情
生物活性：
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy. Apogossypolone also has antifungal activity.
体内研究：
Apogossypolone (ApoG2) (120 mg/kg; i.v. or p.o.; once a day for 5 days) effectively inhibits growth of diffuse large cell lymphoma cells without toxicity.Animal Model:Four-week-old female ICR-SCID mice, each mouse received 107 WSU-DLCL2 cells (in serum-free RPMI 1640) subcutaneously (sc) in each flank area
Dosage:120 mg/kg
Administration:Intravenous or administration per day for five days
Result:Inhibited the growth of WSU-DLCL2 and significantly decreased the tumor weight.
Animal Model:Non-tumor-bearing SCID mice
Dosage:160 mg/kg
Administration:Intravenous or administration per day for five days
Result:Was well tolerated in mice up to 800 mg/kg. Displayed no gross signs of toxicity.
体外研究：
Apogossypolone (ApoG2) shows improved stability under stressed conditions.Apogossypolone (0-1 μM, 72 or 96 h) inhibits WSU-DLCL2 cells growth in a dose-dependent manner.Apogossypolone (0-5 μM, 24 or 48 h) interferes with the formation of heterodimers between anti-apoptotic and pro-apoptotic Bcl-2 family members, and leads to cleavage of caspase-3, caspase-9 and PARP.Apogossypolone (0-8 μM, 0-72 h) induces apoptotic WSU-DLCL2 cell death in a time- and dose-dependent manner.Apogossypolone (0-10 μM, 0-24 h) induces autophagy and promotes ROS generation in HCC cells.
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy. Apogossypolone also has antifungal activity.
体内研究：
Apogossypolone (ApoG2) (120 mg/kg; i.v. or p.o.; once a day for 5 days) effectively inhibits growth of diffuse large cell lymphoma cells without toxicity.Animal Model:Four-week-old female ICR-SCID mice, each mouse received 107 WSU-DLCL2 cells (in serum-free RPMI 1640) subcutaneously (sc) in each flank area
Dosage:120 mg/kg
Administration:Intravenous or administration per day for five days
Result:Inhibited the growth of WSU-DLCL2 and significantly decreased the tumor weight.
Animal Model:Non-tumor-bearing SCID mice
Dosage:160 mg/kg
Administration:Intravenous or administration per day for five days
Result:Was well tolerated in mice up to 800 mg/kg. Displayed no gross signs of toxicity.
体外研究：
Apogossypolone (ApoG2) shows improved stability under stressed conditions.Apogossypolone (0-1 μM, 72 or 96 h) inhibits WSU-DLCL2 cells growth in a dose-dependent manner.Apogossypolone (0-5 μM, 24 or 48 h) interferes with the formation of heterodimers between anti-apoptotic and pro-apoptotic Bcl-2 family members, and leads to cleavage of caspase-3, caspase-9 and PARP.Apogossypolone (0-8 μM, 0-72 h) induces apoptotic WSU-DLCL2 cell death in a time- and dose-dependent manner.Apogossypolone (0-10 μM, 0-24 h) induces autophagy and promotes ROS generation in HCC cells.
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