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品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
H2O: 20 mg/mL, clear
儲存溫度
2-8°C
InChI
1S/C21H26N2O6.ClH/c1-26-17-8-7-13(9-16(17)23-21(25)15(22)12-24)5-6-14-10-18(27-2)20(29-4)19(11-14)28-3;/h5-11,15,24H,12,22H2,1-4H3,(H,23,25);1H
InChI 密鑰
UQNRTPFLTRZEIM-UHFFFAOYSA-N
一般說明
Ombrabulin is a member of the combretastatin A-4 compound class and is a tubulin-depolymerising tumour vascular-disrupting compound.
生化/生理作用
Ombrabulin is a synthetic water-soluble combretastatin analog vascular disrupting agent. Ombrabulin is a tubulin polymerization inhibitor. Ombrabulin binds to the colchicine binding site of endothelial cell tubulin, inhibiting tubulin polymerization and inducing mitotic arrest and apoptosis in endothelial cells.
Ombrabulin leads to the constriction of the arteries, inhibits cell proliferation and causes detachment of endothelial cells, thereby leading to cytotoxicity. In pre-clinical studies, this compound, along with cisplatin, has shown anti-tumor activity. In tumors, it is responsible for the destruction of the vasculature.
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Ombrabulin plus cisplatin versus placebo plus cisplatin in patients with advanced soft-tissue sarcomas after failure of anthracycline and ifosfamide chemotherapy: a randomised, double-blind, placebo-controlled, phase 3 trial.
Lancet Oncology, 16(5), 531-540 (2015)
Phase I safety, pharmacokinetic and pharmacodynamic evaluation of the vascular disrupting agent ombrabulin (AVE8062) in patients with advanced solid tumors.
Clinical Cancer Research, 19(17), 4832-4842 (2013)
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