醌霉素A
| 中文名称 | 醌霉素A |
|---|---|
| 中文同义词 | 棘霉素;醌霉素A;化合物 T15197;棘霉素HIF-1Α抑制剂;QUINOMYCIN A|||NSC-13502 |
| 英文名称 | QUINOMYCIN A |
| 英文同义词 | echinomycina;nsc526417;ECHINOMYCIN;N-[(1R,4S,8R,11S,14R,17S,21R,24S)-3,11,13,16,24,26-hexamethyl-27-methylsulfanyl-2,5,9,12,15,18,22,25-octaoxo-4,17-di(propan-2-yl)-8-(quinoxaline-2-carbonylamino)-6,19-dioxa-28-thia-3,10,13,16,23,26-hexazabicyclo[12.12.3]nonacosan-21-yl]quinoxaline-2-carbo;N-(2-Quinoxalinylcarbonyl)cyclo(D-Ser*-Ala-N-methyl-L-Cys(1)-N-methyl-L-Val-N-(quinoxaline-2-ylcarbonyl)-D-Ser*-Ala-N-methyl-3-methylthio-L-Ala(1)-N-methyl-L-Val-);SK-302B;Echinomycin >97%;N-(2-Quinoxalinylcarbonyl)-O-[N-(2-quinoxalinylcarbonyl)-D-seryl-L-alanyl-3-mercapto-N,S-dimethylcysteinyl-N-methyl-L-valyl]-D-seryl-L-alanyl-N-methylcysteinyl-N-methyl L-valine (81)-lactone cyclic (37)-thioester |
| CAS号 | 512-64-1 |
| 分子式 | C51H64N12O12S2 |
| 分子量 | 1101.26 |
| EINECS号 | |
| 相关类别 | 微生物代谢物;Antitumour;Antibiotic |
| Mol文件 | 512-64-1.mol |
| 结构式 |  |
醌霉素A 性质
| 熔点 | 217-218℃ |
|---|---|
| 比旋光度 | D20 -310° (c = 0.86 in chloroform) |
| 沸点 | 1427.2±65.0 °C(Predicted) |
| 密度 | 1.0964 (rough estimate) |
| 折射率 | 1.6700 (estimate) |
| 储存条件 | -20°C |
| 溶解度 | 溶于DMSO（高达5mg/ml） |
| 酸度系数(pKa) | 9.38±0.70(Predicted) |
| 形态 | 白色固体 |
| 颜色 | 白色至米色 |
| Merck | 13,3531 |
| 稳定性 | 可在-20°C下DMSO溶液中保存长达3个月 |
Echinomycin (Quinomycin A) 是一种有效的,细胞渗透性的低氧诱导因子-1 (HIF-1) DNA 结合活性的小分子抑制剂。Echinomycin 选择性抑制癌症干细胞，其 IC50 值为 29.4 pM。
Echinomycin (0-10 nM; 16 hours; U251 cells) treatment significantly inhibits hypoxia-induced VEGF mRNA expression in a dose-dependent fashion. Echinomycin very potently inhibits hypoxic induction of luciferase expression in U251-HRE in a dose-dependent fashion with an EC 50 of 1.2 nM.
RT-PCR
| Cell Line: | U251 cells |
| Concentration: | 0 nM, 0.625 nM, 1.25 nM, 5 nM, 10 nM |
| Incubation Time: | 16 hours |
| Result: | Significantly inhibited VEGF mRNA expression induced by hypoxia in a dose-dependent fashion. |
Echinomycin (10 μg/kg; intravenous injection; for 40 days; NOD-SCID mice) treatment efficiently eradicates mouse lymphoma and serially transplantable human acute myeloid leukemia (AML) in xenogeneic model by preferential elimination of cancer stem cells (CSCs). HIF1α maintains mouse lymphoma CSCs by repressing a negative feedback loop in the Notch pathway.
| Animal Model: | NOD-SCID mice received 1.8Gy of irradiation and i.v. injection with peripheral blood cells from patients AML-71 and AML-150 |
| Dosage: | 10 μg/kg |
| Administration: | Intravenous injection; for 40 days |
| Result: | Efficiently eradicated mouse lymphoma and serially transplantable human AML in xenogeneic model by preferential elimination of CSCs. |
安全信息
| 危险品标志 | T |
|---|---|
| 危险类别码 | 46-23/24/25 |
| 安全说明 | 53-36/37/39-45 |
| 危险品运输编号 | UN 3462 6.1/PG 2 |
| WGK Germany | 3 |
| RTECS号 | JW5250000 |
| F | 10 |
| 危险等级 | 6.1(b) |
| 包装类别 | III |
| 海关编码 | 2941900000 |
| 提供商 | 语言 |
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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 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-106101 | 醌霉素A Echinomycin | 512-64-1 | 1mg | 3600元 |