奥瑞布林
|
|
|
- CAS号:
- 181816-48-8
- 英文名:
- Ombrabulin
- 英文别名:
- CS-1038;AVE-8062;Ombrabuli;ombrabulin;RPR-258062A.;CS-39-L-Ser.HCl;OMbrabulin(AVE-8062);AVE8062;AC-7700;CS-39-L-SER.HCL;AVE-8062A;AVE-8062;RPR-258062A.;(S,Z)-2-Amino-3-hydroxy-N-(2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl)propanamide;AVE8062; AVE8062A; AC7700; AVE-8062; AVE-8062A; AC-7700; AVE 8062; AVE 8062A; AC 7700
- 中文名:
- 奥瑞布林
- 中文别名:
- 奥瑞布林;(2S)-2-氨基-3-羟基-N-[2-甲氧基-5-[(1Z)-2-(3,4,5-三甲氧基苯基)乙烯基]苯基]丙酰胺
- CBNumber:
- CB31518525
- 分子式:
- C21H26N2O6
- 分子量:
- 402.44
- MOL File:
- 181816-48-8.mol
|
|
|
奥瑞布林化学性质
-
沸点:
-
648.1±55.0 °C(Predicted)
-
|
-
密度:
-
1.258
-
|
-
储存条件:
-
2-8°C
-
|
-
溶解度:
-
Soluble in DMSO
-
|
-
酸度系数(pKa):
-
12.03±0.10(Predicted)
-
|
奥瑞布林性质、用途与生产工艺
奥瑞布林(AVE8062)属于考布他汀(combretastatin)家族，它是抗血管剂(或VDA即血管破坏剂)。奥瑞布林可按碱形式或按药用酸的盐形式例如按以下盐酸盐形式给药，一旦给药，奥瑞布林就在体内释放活性代谢产物(Z)‑1‑(3‑氨基‑4‑甲氧基 苯基)‑2‑(3,4,5‑三甲氧基苯基)乙烯，因此，也可用呈碱形式或呈药用酸的盐形式的具有下式的另一种考布他汀代替奥瑞布林。
奥瑞布林可与多西紫杉醇和顺铂联用。在这种情况下，可将奥瑞布林以20mg/m2的剂量、多西紫杉醇以75mg/m2的剂量及顺铂以75mg/m2 的剂量给药。在这种情况下，也可将奥瑞布林以35mg/m2的剂量、多西紫杉 醇以75mg/m2的剂量及顺铂以75mg/m2的剂量给药。
Ombrabulin (AVE8062) 是 CA-4 磷酸酯的衍生物，选择性破坏内皮细胞的微管蛋白细胞骨架，具有抗血管作用。
The effect of Ombrabulin (AC-7700) on endothelial or tumor cell viability is examined using the MTT assay. The IC
50
of Ombrabulin for the mouse mesenteric endothelial cells (MMEC) is 10 nM and ranges between 7 and 20 nM for the tumor cell lines (HeyA8, SKOV3ip1, and HeyA8-MDR). Comparative analysis of the nonlinear least-squares regression of the dose-response curves for each agent alone and combination Ombrabulin (AC-7700)/Docetaxel show a significantly lower IC
50
than either agent alone (P<0.005, all cell lines). The cytotoxicity of Docetaxel is 2- to 4-fold greater in combination with Ombrabulin (AC-7700) for the endothelial and tumor cells compared with Docetaxel alone.
Before performing therapy experiments, the tolerability of various doses of Ombrabulin (AC-7700) ranging from 10 to 100 mg/kg is tested given twice weekly via i.v., i.p., or s.c. routes in nude mice (n=3 per group). The i.v. and s.c. routes are not pursued further due to problems with skin or tail vein necrosis. The i.p. route is well tolerated with doses up to 100 mg/kg. Next, preliminary experiments are done to determine the lowest dose for in vivo therapeutic efficacy. Starting 7 days after tumor cell injection, nude mice (n=5 per group) bearing HeyA8 ovarian cancer cells are treated with either vehicle or Ombrabulin 10, 30, 50, and 100 mg/kg twice weekly i.p. for 3 weeks. There is 65% reduction in tumor weight in the 30 mg/kg group compared with the vehicle control group (P<0.02). The 10 mg/kg dose is not effective. The antitumor effects at doses >30 mg/kg are not significantly better; therefore, the 30 mg/kg dose is selected for subsequent therapy experiments.
奥瑞布林
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-14797 | Ombrabulin | | 5 mg | 1000元 |
| 2024/01/25 | HY-14797 | Ombrabulin | | 10 mg | 1600元 |
181816-48-8, 奥瑞布林 相关搜索:
- 标准品
- 标准品 -中药标准品
- 植物提取物
- 奥瑞布林
- (2S)-2-氨基-3-羟基-N-[2-甲氧基-5-[(1Z)-2-(3,4,5-三甲氧基苯基)乙烯基]苯基]丙酰胺
- 181816-48-8
- Ombrabuli
- (S,Z)-2-Amino-3-hydroxy-N-(2-methoxy-5-(3,4,5-trimethoxystyryl)phenyl)propanamide
- (2S)-2-amino-3-hydroxy-N-[2-methoxy-5-[(Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl]propanamide
- AVE8062; AVE8062A; AC7700; AVE-8062; AVE-8062A; AC-7700; AVE 8062; AVE 8062A; AC 7700
- CS-1038
- RPR-258062A.
- CS-39-L-Ser.HCl
- AVE8062;AC-7700;CS-39-L-SER.HCL;AVE-8062A;AVE-8062;RPR-258062A.
- OMbrabulin(AVE-8062)
- AVE-8062
- PropanaMide,2-aMino-3-hydroxy-N-[2-Methoxy-5-[(1Z)-2-(3,4,5-triMethoxyphenyl)ethenyl]phenyl]-,(2S)-
- (2S)-2-Amino-3-hydroxy-N-[2-methoxy-5-[(1Z)-2-(3,4,5-trimethoxyphenyl)ethenyl]phenyl]propanamide
- ombrabulin