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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Cytoskeleton > Combretastatin A4CAS：117048-59-6
Molecular Formula：C18H20O5
Molecular Weight：316.35
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 117048-59-6 |
| Name | Combretastatin A4 |
| Molecular Formula | C18H20O5 |
| Molecular Weight | 316.35 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD03453309 |
| SMILES | OC1=CC(/C=C\C2=CC(OC)=C(OC)C(OC)=C2)=CC=C1OC |
| Target Point | Microtubule/Tubulin |
| Passage | Cytoskeleton |
| Background | Combretastatin A4 is a microtubule inhibitor capable of binding to β-tubulin. |
| Biological Activity | Combretastatin A4 是一种 microtubule 抑制剂，能够与 β-tubulin 结合，Kd 值为 0.4 μM[1-4]。 |
| In Vitro | Combretastatin A4磷酸盐(≥50μM)显著增加膜联蛋白-V结合细胞的百分比并显著降低前向散射。 Combretastatin A4磷酸盐不会明显增加溶血。百μMCombretastatin A4磷酸盐显著增加Fluo3荧光。通过去除细胞外Ca 2+，Combretastatin A4磷酸盐(100μM)对膜联蛋白-V结合的影响显著减弱，但未消除。 Combretastatin A4磷酸盐(≥50μM)显著降低GSH丰度和ATP水平，但不显著增加ROS或神经酰胺[2]。聚合物囊泡共同包裹多柔比星 - combretastatin-A4磷酸盐(1:10)显示出对人鼻咽表皮癌(KB)细胞的强协同细胞毒作用[3]。用Combretastatin A4磷酸盐预处理不影响3-D培养物中VM的量以及这些关键分子的表达[4]。 |
| In Vivo | 施用30分钟后DBP和MBP在用Combretastatin A4磷酸二钠120mg/10mL/kg处理的大鼠中更高。表明Combretastatin A4磷酸盐和Combretastatin A4在用Combretastatin A4磷酸二钠120 mg/10 mL/kg处理的大鼠中的毒代动力学参数，Combretastatin A4的Cmax，T1/2和AUC0-inf值为156±13μM，5.87±1.69 h，和89.4±10.1 h·μM，分别为[1]。在体内，W256肿瘤在Combretastatin A4磷酸盐处理后显示出显著的肿瘤内缺氧，伴随着VM形成的增加。 Combretastatin A4磷酸盐在2天内仅表现出肿瘤生长的延迟，但随后肿瘤迅速再生。在第8天，VM密度与肿瘤体积和肿瘤重量正相关.Combretastatin A4磷酸盐引起缺氧，其通过HIF-1α/ EphA2/PI3K /基质金属蛋白酶(MMP)信号传导途径诱导W256肿瘤中的VM形成，导致随后的再生长。受损的肿瘤[4]。 |
| Animal Experiment | 大鼠：通过推注输注给大鼠单次静脉内剂量的Combretastatin A4磷酸二钠120mg/10mL/kg(n = 3)。通过颈静脉取血并在给药后10分钟和1，3，6和24小时收集在肝素涂覆的管中。取样后立即通过离心分离血浆。离心后，将等分试样的血浆与等体积的1％甲酸混合并储存在-20℃。通过固相萃取纯化解冻的血浆样品，测定combretastatin A4磷酸盐(Combretastatin A4磷酸二钠的游离碱; Combretastatin A4磷酸盐)和combretastatin A4(Combretastatin A4磷酸二钠的代谢物; Combretastatin A4)的血浆浓度。通过液相色谱 - 串联质谱(LC-MS/MS)。使用Phoenix WinNonlin 6.3通过非区室分析获得毒性动力学参数[最大浓度(C max)，终末半衰期(T1/2)和从0时间到无穷大的浓度 - 时间曲线下面积(AUC 0-inf)]。 |
| Data Literature Source | [1]. Tochinai R，et al. Combretastatin A4 disodium phosphate-induced myocardial injury. J Toxicol Pathol. 2016 Jul;29(3):163-71. [2]. Signoretto E，et al. Stimulation of Eryptosis by Combretastatin A4 Phosphate Disodium (CA4P). Cell Physiol Biochem. 2016;38(3):969-81 [3]. Zhu J，et al. Co-Encapsulation of Combretastatin-A4 Phosphate and Doxorubicin in Polymersomes for Synergistic Therapy of Nasopharyngeal Epidermal Carcinoma. J Biomed Nanotechnol. 2015 Jun;11(6):997-1006. [4]. Yao N，et al. Combretastatin A4 phosphate treatment induces vasculogenic mimicry formation of W256 breast carcinoma tumor in vitro and in vivo. Tumour Biol. 2015 Nov;36(11):8499-510. |
| Unit | Piece |
| Specification | 5mg 10mM*1mL in DMSO 10mg 20mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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Positioning Remodeling Nanogels Mediated Codelivery of Antivascular Drug and Autophagy Inhibitor for Cooperative Tumor Therapy
Click to check >>Author：Zhang H. Ren Y. Hou L. Chang J. Zhang Z. Zhang H
IF：8.7480
Publish_to：ACS Appl Mater Interfaces
PMID：31951366
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