變棉子酚
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- CAS號(hào):
- 66389-74-0
- 英文名:
- apogossypol
- 英文別名:
- NSC736630;apogossypol;(+)-APOGOSSYPOL;APOGOSSYPOL;NSC736630;(+)Apogossypol,(+) Apogossypol;(+)-3,3'-Dimethyl-5,5'-bis(1-methylethyl)-2,2'-binaphthalene-1,1',6,6',7,7'-hexol;[2,2'-Binaphthalene]-1,1',6,6',7,7'-hexol, 3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2S)-;3-methyl-5-propan-2-yl-2-(1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,6,7-triol
- 中文名:
- 變棉子酚
- 中文別名:
- 變棉子酚;變棉子酚;阿樸棉子酚;化合物 T13459;化合物 (+)-APOGOSSYPOL
- CBNumber:
- CB21268526
- 分子式:
- C28H30O6
- 分子量:
- 462.53
- MOL File:
- 66389-74-0.mol
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變棉子酚化學(xué)性質(zhì)
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熔點(diǎn):
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118-123 °C
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沸點(diǎn):
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673.3±50.0 °C(Predicted)
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密度:
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1.335±0.06 g/cm3(Predicted)
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儲(chǔ)存條件:
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Store at -20°C
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溶解度:
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>16.2mg/mL in DMSO with gentle warming
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形態(tài):
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Powder
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酸度系數(shù)(pKa):
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8.03±0.50(Predicted)
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變棉子酚性質(zhì)、用途與生產(chǎn)工藝
(+)-Apogossypol 是一種泛 BCL-2 拮抗劑，與 Mcl-1, Bcl-2 和 Bcl-xL 結(jié)合， EC50 分別為 2.6，2.8 和 3.69 μM。
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Mcl-1
2.6 μM (EC
50
)
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Bcl-2
2.8 μM (EC
50
)
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Bcl-xL
3.69 μM (EC
50
)
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In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with K
d
values of 1.7 μM.To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed. The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol. The concentration for 50% inhibition (IC
50
) on LNCaP cells within ~72 h is 9.57 μM, while the IC
50
of Gossypol on LNCaP cells is 10.35 μM.
Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant anti-growth and anti-tumor activities in vitro, similar to those of Gossypol. The anti-cancer effect of (+)-Apogossypol is evaluated in mice bearing subcutaneous LNCaP cell xenografts. The tumor growth is monitored and measured by a caliper and balance. The survival rate of the mice is notably improved by (+)-Apogossypol. Of note, the tumor sizes are also markedly decreased by (+)-Apogossypol treatment (P<0.01).
變棉子酚
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66389-74-0, 變棉子酚 相關(guān)搜索:
- 抑制劑
- 化合物 (+)-APOGOSSYPOL
- 化合物 T13459
- 變棉子酚
- 變棉子酚
- 阿樸棉子酚
- 66389-74-0
- (+)Apogossypol,(+) Apogossypol
- [2,2'-Binaphthalene]-1,1',6,6',7,7'-hexol, 3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2S)-
- (+)-APOGOSSYPOL
- 3-methyl-5-propan-2-yl-2-(1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,6,7-triol
- APOGOSSYPOL;NSC736630
- NSC736630
- (+)-3,3'-Dimethyl-5,5'-bis(1-methylethyl)-2,2'-binaphthalene-1,1',6,6',7,7'-hexol
- apogossypol