中文名 | Rottlerin |
英文名 | Rottlerin |
别名 | 咖马林 罗特林 粗糠柴毒素 粗糠紫苦素 粗糠柴苦素 化合物DIBAC4(3) |
英文别名 | kamalin Rottlerin ROTTLERIN MALLOTOXIN 4',6'-trihydroxy-5'-methyl-methyl)-2 acetophenone,3'-((8-cinnamoyl-5,7-dihydroxy-2,2-dimethyl-2h-1-benzopyran-6-yl) 3'-[(8-CINNAMOYL-5,7-DIHYDROXY-2,2-DIMETHYL-2H-1-BENZOPYRAN-6-YL)METHYL]-2',4',6'-TRIHYDROXY-5'-METHYLACETOPHENONE 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 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)- |
CAS | 82-08-6 |
EINECS | 201-395-4 |
化学式 | C30H28O8 |
分子量 | 516.54 |
密度 | 1.2051 (rough estimate) |
熔点 | 200 °C |
沸点 | 521.39°C (rough estimate) |
溶解度 | 溶于DMSO (高达50 mg/ml)。 |
折射率 | 1.4900 (estimate) |
酸度系数 | 6.92±0.40(Predicted) |
存储条件 | 2-8°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO中的溶液可以在-20 ° 下储存长达1个月。 |
外观 | 粉末 |
颜色 | Orange to brown |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xn - 有害物品 |
风险术语 | R20/21/22 - 吸入、皮肤接触及吞食有害。 R22 - 吞食有害。 |
安全术语 | S36/37 - 穿戴适当的防护服和手套。 S24/25 - 避免与皮肤和眼睛接触。 |
WGK Germany | 3 |
RTECS | AM6913800 |
海关编号 | 29329990 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.936 ml | 9.68 ml | 19.36 ml |
5 mM | 0.387 ml | 1.936 ml | 3.872 ml |
10 mM | 0.194 ml | 0.968 ml | 1.936 ml |
5 mM | 0.039 ml | 0.194 ml | 0.387 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!