| Identification | Back Directory | [Name]
[2,2'-Binaphthalene]-1,1',4,4'-tetrone, 6,6',7,7'-tetrahydroxy-3,3'-diMethyl-5,5'-bis(1-Methylethyl)- | [CAS]
886578-07-0 | [Synonyms]
APOG2
Apogossypolone
Apogossypolone (ApoG2)
Gossypol Derivative ApoG2
[2,2'-Binaphthalene]-1,1',4,4'-tetrone, 6,6',7,7'-tetrahydroxy-3,3'-diMethyl-5,5'-bis(1-Methylethyl)- | [Molecular Formula]
C28H26O8 | [MOL File]
886578-07-0.mol | [Molecular Weight]
490.5 |
| Chemical Properties | Back Directory | [Melting point ]
>185°C (dec.) | [storage temp. ]
Refrigerator | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
Dark Yellow to Dark Orange |
| Hazard Information | Back Directory | [Uses]
Apogossypolone is an anticancer agent that induces apoptosis in carcinoma cells. Antiproliferative. | [Biological Activity]
apogossypolone is an inhibitor of bcl-2, mcl-1 and bcl-xl with ki values of 35nm, 25nm and 660nm, respectively [1].the mtt-based cell cytotoxicity assay shows that apogossypolone has an anticancer activity with ic50 values of 1, 2 and 3μm, respectively in pc-3, du-145 (human prostate cancer cell lines) and mda-mb-231(human breast cancer cell line). apogossypolone is also found to inhibit the colony formation of du-145 cells. the mechanism is that apogossypolone binds to bcl-2 and prevents its association with bh3-only pro-apoptotic proteins, leading the pro-apoptotic proteins to participate in the apoptotic response [2].besides prostate cancer and breast cancer, apogossypolone is also potent in follicular lymphoma. apogossypolone significantly inhibits the cell growth via inducing apoptosis in wsu-fsccl cell line with ic50 value of 109.2nm at 72h [3]. | [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 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. |
| [target]
Bcl-2 | [IC 50]
Mcl-1: 25 nM (Ki); Bcl-2: 35 nM (Ki); Bcl-xL: 660 nM (Ki) | [References]
[1] zhang xq, huang xf, hu xb, zhan yh, an qx, yang sm, xia aj, yi j, chen r, mu sj, wu dc. apogossypolone, a novel inhibitor of antiapoptotic bcl-2 family proteins, induces autophagy of pc-3 and lncap prostate cancer cells in vitro. asian j androl. 2010 sep;12(5):697-708.
[2] zhan y, jia g, wu d, xu y, xu l. design and synthesis of a gossypol derivative with improved antitumor activities. arch pharm (weinheim). 2009 apr;342(4):223-9.
[3] arnold aa, aboukameel a, chen j, yang d, wang s, al-katib a, mohammad rm. preclinical studies of apogossypolone: a new nonpeptidic pan small-molecule inhibitor of bcl-2, bcl-xl and mcl-1 proteins in follicular small cleaved cell lymphoma model. mol cancer. 2008 feb 14;7:20. |
| Spectrum Detail | Back Directory | [Spectrum Detail]
[2,2'-Binaphthalene]-1,1',4,4'-tetrone, 6,6',7,7'-tetrahydroxy-3,3'-diMethyl-5,5'-bis(1-Methylethyl)-(886578-07-0)MS
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| Company Name: |
Creative Enzymes
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| Tel: |
1-516-855-7709 |
| Website: |
www.creative-enzymes.com |
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