埃博霉素A

更新时间：2024-01-02 18:39:02

埃博霉素A结构式	常用名	埃博霉素A	英文名	Epothilone A
	CAS号	152044-53-6	分子量	493.656
	密度	1.1±0.1 g/cm3	沸点	683.3±55.0 °C at 760 mmHg
	分子式	C₂₆H₃₉NO₆S	熔点	95ºC
	MSDS	中文版美版	闪点	367.1±31.5 °C

埃博霉素A用途

Epothilone A 是紫杉醇和管蛋白 (tubulin) 聚合物结合的竞争性抑制剂,其 Ki 值为 0.6-1.4 μM。

中文名	埃博霉素 A
英文名	(1R,5S,6S,7R,10S,14S,16S)-6,10-dihydroxy-5,7,9,9-tetramethyl-14-[(E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-13,17-dioxabicyclo[14.1.0]heptadecane-8,12-dione
中文别名	埃博霉素A \| 西洛他唑
英文别名	更多

描述	Epothilone A 是紫杉醇和管蛋白 (tubulin) 聚合物结合的竞争性抑制剂,其 Ki 值为 0.6-1.4 μM。
相关类别	信号通路 >> 细胞周期/DNA损伤 >> 微管/微管蛋白信号通路 >> 细胞骨架 >> 微管/微管蛋白研究领域 >> 癌症天然产物 >> 其他
体外研究	埃坡霉素A是[3H]紫杉醇与微管蛋白聚合物结合的竞争性抑制剂。通过Hanes分析,Epothilone A的表观Ki值为1.4μM,Dixon分析的表观Ki值为0.6μM[1]。当应用于人T-24膀胱癌细胞系时,埃坡霉素A在体外具有高度细胞毒性(IC 50 =0.05μM)。基于竞争测定,埃坡霉素A与微管蛋白的结合亲和力与紫杉醇对微管蛋白的结合亲和力具有相同的数量级。从微管蛋白结合位点取出100nM(3H)紫杉醇的IC50对于紫杉醇为3.6μM,对于埃坡霉素A为2.3μM,对于patupilone为3.3μM[2]。
参考文献	[1]. Kowalski RJ, et al. Activities of the microtubule-stabilizing agents epothilones A and B with purified tubulin and in cells resistant to paclitaxel (Taxol(R)). J Biol Chem. 1997 Jan 24;272(4):2534-41. [2]. Cheng KL, et al. Novel microtubule-targeting agents - the epothilones. Biologics. 2008 Dec;2(4):789-811.

密度	1.1±0.1 g/cm3
沸点	683.3±55.0 °C at 760 mmHg
熔点	95ºC
分子式	C₂₆H₃₉NO₆S
分子量	493.656
闪点	367.1±31.5 °C
精确质量	493.249817
PSA	137.49000
LogP	2.54
蒸汽压	0.0±2.2 mmHg at 25°C
折射率	1.532
储存条件	-20°C

危险品运输编码	NONH for all modes of transport

埃博霉素A上游产品 7
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埃博霉素A下游产品 1
CAS号186692-73-9 埃博霉素 C

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Conformational preferences of natural and C3-modified epothilones in aqueous solution.

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The conformational properties of the microtubule-stabilizing agent epothilone A ( 1a) and its 3-deoxy and 3-deoxy-2,3-didehydro derivatives 2 and 3 have been investigated in aqueous solution by a comb...

UNII-51E07YBX96

Epothilone A

(-)-Epothilone A

Epo A

4,17-Dioxabicyclo[14.1.0]heptadecane-5,9-dione, 7,11-dihydroxy-8,8,10,12-tetramethyl-3-[(E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-, (1S,3S,7S,10R,11S,12S,16R)-

[1R*,3R*(E),7R*,10S*,11R*,12R*,16S*]-7,11-dihydroxy-8,8,10,12-tetramethyl-3-[1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione

Epothilon A

(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12-tetramethyl-3-[(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione

(1S,3S,7S,10R,11S,12S,16R)-7,11-Dihydroxy-8,8,10,12-tetramethyl-3-[(1E)-1-(2-methyl-1,3-thiazol-4-yl)-1-propen-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione

4,17-Dioxabicyclo[14.1.0]heptadecane-5,9-dione, 7,11-dihydroxy-8,8,10,12-tetramethyl-3-[(E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-, (1R,3R,7R,10S,11R,12R,16S)-

(1R,3R,7R,10S,11R,12R,16S)-7,11-Dihydroxy-8,8,10,12-tetramethyl-3-[(1E)-1-(2-methyl-1,3-thiazol-4-yl)-1-propen-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione

epithilone A

Epothilones

(1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12-tetramethyl-3-[(1E)-1-(2-methyl-1,3-thiazol-4-yl)prop-1-en-2-yl]-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione