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Apogossypolone (Synonyms: ApoG2)
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。
Apogossypolone Chemical Structure
CAS No. : 886578-07-0
| 规格 |
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是否有货 |
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| 100 mg |
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询价 |
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| 250 mg |
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询价 |
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| 500 mg |
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询价 |
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* Please select Quantity before adding items.
| 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[1] and autophagy[2]. Apogossypolone also has antifungal activity[3].
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| IC50 & Target |
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Mcl-1
25 nM (Ki)
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Bcl-2
35 nM (Ki)
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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-DLCL2 cells 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-DLCL2 cell 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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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-XL and 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].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
| 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[1] |
| 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[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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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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| 参考文献 |
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[1]. Yuan Sun, et al. Apogossypolone, a nonpeptidic small molecule inhibitor targeting Bcl-2 family proteins, effectively inhibits growth of diffuse large cell lymphoma cells in vitro and in vivo. Cancer Biol Ther. 2008 Sep;7(9):1418-26.
[2]. Cheng P, et al. The novel BH-3 mimetic apogossypolone induces Beclin-1- and ROS-mediated autophagy in human hepatocellular carcinoma [corrected] cells. Cell Death Dis. 2013 Feb 7;4(2):e489.
[3]. Jay E Mellon, et al. Inhibitory effects of gossypol, gossypolone, and apogossypolone on a collection of economically important filamentous fungi. J Agric Food Chem. 2012 Mar 14;60(10):2740-5.
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