中文名 | 巨大戟醇-3-O-当归酸酯 |
英文名 | Ingenol-3- angelate |
别名 | 3-当归酰巨大戟萜醇 巨大戟醇-3-当归酸酯 巨大戟醇-3-O-当归酸酯 巨大戟醇-3-O-当归酸酯(巨大戟醇甲基丁烯酸酯) |
英文别名 | I3A PEP005 Picato Ingenol mebutate INGENOL MEBUTATE Ingenol 3-mebutate Ingenol-3- angelate Ingenol-3-O-angelate Ingenol Mebutate (PEP005) Ingenol-3-O-angelate 75567-37-2 (2Z)-2-Methyl-2-butenoic acid (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2,5,5a,6,9,10,10a-octahydro-5,5a-dihydroxy-4-(hydroxymethyl)-1,1,7,9-tetramethyl-11-oxo-1H-2,8a-methanocyclopenta[a]cyclopropa[e]cyclodecen-6-yl ester |
CAS | 75567-37-2 |
化学式 | C25H34O6 |
分子量 | 430.53 |
密度 | 1.26±0.1 g/cm3(Predicted) |
沸点 | 576.9±50.0 °C(Predicted) |
水溶性 | Soluble in 100% ethanol, DMSO, dichloromethane, and methanol. Insoluble in water. |
溶解度 | DMSO: 可溶15mg/mL,澄清 |
酸度系数 | 11.52±0.70(Predicted) |
存储条件 | -20°C |
稳定性 | 稳定1年的供应。DMSO或乙醇中的溶液可以在-20 °C下储存长达1个月。 |
外观 | 粉末 |
颜色 | white to beige |
物化性质 | 白色粉末,可溶于甲醇、乙醇、DMSO等有机溶剂,来源于大戟科(Euphorbia)植物的全草。 |
MDL号 | MFCD07784504 |
体外研究 | Ingenol Mebutate (Ingenol 3-angelate) is an active ingredient in Euphorbia peplus , acting as a potent PKC activator, with K i s of 0.3, 0.105, 0.162, 0.376, and 0.171 nM for PKC-α, PKC-β, PKC-γ, PKC-δ, and PKC-ε, respectively. Ingenol Mebutate also EC 50 s of 13 ± 2.4 nM (PKC-α), 4.37 ± 0.4 nM (PKC-βI), 10.5 ± 2.2 nM (PKC-βII), 38.6 ± 2.9 nM (PKC-δ), 1.08 ± 0.01 nM (PKC-ε), 0.9 ± 0.13 nM (PKC-μ) in WEHI-231 cells, 198 ± 12.5 nM (PKC-α), 69.1 ± 8.2 nM (PKC-βI), 4.6 ± 0.4 nM (PKC-ε) and 1 nM (PKC-μ) in HOP-92 cells, 635 ± 245 nM (PKC-α), 146 ± 35 nM (PKC-βI), 4.7 ± 0.7 nM (PKC-δ), 1.1 ± 0.5 nM (PKC-ε), and 30 nM (PKC-μ) in Colo-205 cells. Ingenol Mebutate sensitizes WEHI-231 cells, HOP-92 and Colo-205 cells, with IC 50 s of 1.41 ± 0.255 nM, 3.24 ± 2.01 nM, and 11.9 ± 1.307 nM, respectively. Ingenol Mebutate (PEP005; 20 nM) actions are PKC-δ dependent, induces apoptosis in primary AML marrow blasts but not in normal myeloblasts. Ingenol Mebutate (PEP005) activates PKCδ and inhibits PKCα. Colo205-R cells (IC 50 : >10 μM) are >300-fold more resistant to Ingenol Mebutate than parental Colo205-S cells. |
下游产品 | 巨大戟醇 |
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