粗糠柴苦素
中文名称 | 粗糠柴苦素 |
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中文同义词 | 粗糠紫苦素;咖马林/粗糠柴苦素;咖马林;粗糠柴苦素;粗糠柴毒素;罗特林;化合物DIBAC4(3);(E)-1-(6-(3-乙酰基-2,4,6-三羟基-5-甲基苄基)-5,7-二羟基-2,2-二甲基-2H-苯并吡喃-8-己)-3-苯基丙-2-烯-1-酮 |
英文名称 | ROTTLERIN |
英文同义词 | 3'-[(8-CINNAMOYL-5,7-DIHYDROXY-2,2-DIMETHYL-2H-1-BENZOPYRAN-6-YL)METHYL]-2',4',6'-TRIHYDROXY-5'-METHYLACETOPHENONE;4’,6’-trihydroxy-5’-methyl-methyl)-2;acetophenone,3’-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-6-yl);2-Propen-1-one, 1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-, (2E)-;1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one;(E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one;Rottlerin,98%;Rottlerin, 98% 10MG |
CAS号 | 82-08-6 |
分子式 | C30H28O8 |
分子量 | 516.54 |
EINECS号 | 201-395-4 |
相关类别 | 植物提取物;合成材料中间体;试剂盒-细胞分析试剂盒;Aromatic Phenols;Protein Kinase |
Mol文件 | 82-08-6.mol |
结构式 |
粗糠柴苦素 性质
熔点 | 200 °C |
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沸点 | 521.39°C (rough estimate) |
密度 | 1.2051 (rough estimate) |
折射率 | 1.4900 (estimate) |
储存条件 | 2-8°C |
溶解度 | 溶于DMSO(高达50mg/ml)。 |
形态 | 粉末 |
酸度系数(pKa) | 6.92±0.40(Predicted) |
颜色 | 橙色至棕色 |
稳定性 | DMSO中的溶液可在-20°下稳定储存1个月。 |
LogP | 8.660 (est) |
CAS 数据库 | 82-08-6(CAS DataBase Reference) |
Target | Value |
PKCδ
(Cell-free assay) | 3 μM |
CKIII
(Cell-free assay) | 5.3 μM |
PKCα
(Cell-free assay) | 30 μM |
CKII
(Cell-free assay) | 30 μM |
PKCγ
(Cell-free assay) | 40 μM |
Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC.
Rottlerin (20 μM) exhibits cell proliferation in HMVEC.
Western Blot Analysis
Cell Line: | Primary HMVEC (Human Microvascular Endothelial Cell). |
Concentration: | 20 μM. |
Incubation Time: | 2, 6, 24 hours. |
Result: | Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h. |
Cell Proliferation Assay
Cell Line: | Primary HMVEC (Human Microvascular Endothelial Cell). |
Concentration: | 20 μM. |
Incubation Time: | 24/48 hours. |
Result: | Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively. |
Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity.
Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP).
Animal Model: | Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×10 6 cells mixed with Matrigel, 50:50 ratio) injection. |
Dosage: | 0 or 20 mg/kg. |
Administration: | Gavage 5 days per week, once daily, for 6 weeks. |
Result: | Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect on the body weight of AsPC-1 tumor-bearing mice. |
安全信息
危险品标志 | Xn |
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危险类别码 | 20/21/22-22 |
安全说明 | 36/37-24/25 |
WGK Germany | 3 |
RTECS号 | AM6913800 |
海关编码 | 29329990 |
提供商 | 语言 |
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英文
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英文
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | C32849 | 粗糠柴毒素 Rottlerin, 98% | 82-08-6 | 10mg | 1818元 |
2024/04/30 | HY-18980 | Rottlerin | 5 mg | 812元 |