Apogossypolone (ApoG2) 是一种具有口服活性的Bcl-2 family proteins抑制剂，对 Bcl-2, Mcl-1 和 Bcl-XL的Ki值分别为 35, 25 和 660 nM。Apogossypolone 具有抗肿瘤活性，诱导细胞凋亡 (apoptosis) 和 自噬 (autophagy)。Apogossypolone 具有抗真菌活性。
| 生物活性 | Apogossypolone (ApoG2) is an orally activeBcl-2 familyproteinsinhibitor withKivalues of 35, 25 and 660 nM forBcl-2,Mcl-1and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cellapoptosis[1]andautophagy[2]. Apogossypolone also has antifungal activity[3]. |
| IC50& Target | Mcl-1 25 nM (Ki) | Bcl-2 35 nM (Ki) | Bcl-xL 660 nM (Ki) |
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体外研究
(In Vitro) | Apogossypolone (ApoG2) shows improved stability under stressed conditions[1].
Apogossypolone (0-1 μM, 72 or 96 h) inhibits WSU-DLCL2cells growth in a dose-dependent manner[1].
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[1].
Apogossypolone (0-8 μM, 0-72 h) induces apoptotic WSU-DLCL2cell death in a time- and dose-dependent manner[1].
Apogossypolone (0-10 μM, 0-24 h) induces autophagy and promotes ROS generation in HCC cells[2].
Cell Proliferation Assay[1] | Cell Line: | WSU-DLCL2 | | Concentration: | 250, 350, 500 and 1000 nM | | Incubation Time: | 96 h for cell counting, 72 h for MTT | | Result: | Inhibited growth in a dose-dependent manner. The 50% growth inhibition concentration (IC50) was approximately 350 nM. |
Western Blot Analysis[1] | Cell Line: | WSU-DLCL2 | | Concentration: | 0.35, 0.5, 1 and 5 μM | | Incubation Time: | 24 or 48 h | | Result: | Blocked the formation of heterodimers between Bcl-XLand Bim in a concentration-dependent manner. Resulted in the activation of cleavages of caspase-3, caspase-9 and PARP. |
Apoptosis Analysis[1] | Cell Line: | WSU-DLCL2 | | Concentration: | 0, 1, 2, 4 and 8 μM | | Incubation Time: | 24, 48 and 72 h | | Result: | Induced cell apoptosis in a time- and dose-dependent manner. |
Cell Autophagy Assay[2] | Cell Line: | HepG2 and Hep3B | | Concentration: | 1.25, 2.5, 5 and 10 μM | | Incubation Time: | 6, 12, 18 and 24 h | | Result: | Induced LC3 (Light chain 3)-II conversion in a dose- and time-dependent manner. |
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体内研究
(In Vivo) | 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[1].
| Animal Model: | Four-week-old female ICR-SCID mice, each mouse received 107WSU-DLCL2cells (in serum-free RPMI 1640) subcutaneously (sc) in each flank area[1] | | Dosage: | 120 mg/kg | | Administration: | Intravenous or administration per day for five days | | Result: | Inhibited the growth of WSU-DLCL2and significantly decreased the tumor weight. |
| Animal Model: | Non-tumor-bearing SCID mice[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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