AVE8062A
- CAS号:253426-24-3
- 英文名:AVE8062A
- 中文名:AVE8062A
- CBNumber:CB42522391
- 分子式:C21H27ClN2O6
- 分子量:438.91
- MOL File:253426-24-3.mol
- 储存条件 :2-8°C
- 溶解度 :DMSO: soluble; Ethanol: soluble
- 形态 :powder
- 颜色 :white to beige
- RTECS号 :TX1404540
AVE8062A性质、用途与生产工艺
- 生物活性 Ombrabulin hydrochloride 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。
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靶点
tubulin
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体外研究
The effect of Ombrabulin (AVE8062) 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 /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 for the endothelial and tumor cells compared with Docetaxel alone.
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体内研究
Before performing therapy experiments, the tolerability of various doses of Ombrabulin (AVE8062) 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.
- 更新日期:2024/11/08
- 产品编号:HY-18256
- 产品名称:AVE8062A Ombrabulin hydrochloride
- CAS编号:253426-24-3
- 包装:5mg
- 价格:1000元
- 更新日期:2024/11/08
- 产品编号:HY-18256
- 产品名称:Ombrabulin hydrochloride
- CAS编号:
- 包装:10 mM * 1 mLin DMSO
- 价格:1100元
- 公司名称:MedChemexpress LLC
- 联系电话:021-58955995
- 电子邮件:sales@medchemexpress.cn
- 国家:美国
- 产品数:4861
- 优势度:58
- 公司名称:Musechem
- 联系电话:+1-800-259-7612
- 电子邮件:info@musechem.com
- 国家:美国
- 产品数:4660
- 优势度:60
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:+1-781-999-5354 +1-00000000000
- 电子邮件:marketing@targetmol.com
- 国家:美国
- 产品数:32161
- 优势度:58
- 公司名称:TargetMol Chemicals Inc.
- 联系电话:
- 电子邮件:support@targetmol.com
- 国家:美国
- 产品数:38631
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- 公司名称:Aladdin Scientific
- 联系电话:+1-+1(833)-552-7181
- 电子邮件:sales@aladdinsci.com
- 国家:美国
- 产品数:52924
- 优势度:58
- 公司名称:CAYMAN
- 联系电话:--
- 电子邮件:cayman@caymanchem.com
- 国家:美国
- 产品数:6213
- 优势度:81
- 公司名称:MedChemExpress
- 联系电话:--
- 电子邮件:sales@medchemexpress.com
- 国家:美国
- 产品数:6398
- 优势度:58