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Combretastatin A4
中文名稱：康普立停 A4
Combretastatin A4 是一種以 microtubule 為靶點的試劑，其與β-微管蛋白結合，Kd 為 0.4 μM。Phase 3。
Combretastatin A4 Chemical Structure
CAS: 117048-59-6
產品質控
批次：
S778301
DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false
純度：
99.87%
99.87
Combretastatin A4相關產品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM | ||
| SK-OV-3 | Growth inhibition assay | 48 h | Growth inhibition of human SK-OV-3 after 48 hrs by SRB assay, GI50=0.00013 μM | ||
| KBV1 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM | ||
| SK-N-BE | Proliferation assay | 72 h | Antiproliferative activity in human SK-N-BE cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00058 μM | ||
| NCIH460 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM | ||
| KB-VIN10 cells | Proliferation assay | 72 h | Antiproliferative activity against human KB-VIN10 cells over-expressing P-gp 170/MDR1 after 72 hrs by methylene blue assay, IC50=0.0007 μM | ||
| HCT116 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells assessed as reduction of [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50=0.00074 μM | ||
| DU145 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM | ||
| RS4:11 cells | Proliferation assay | 72 h | Antiproliferative activity against human RS4:11 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.0008 μM | ||
| HeLa cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM | ||
| Calu6 | Proliferation assay | 48 h | Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM | ||
| HCT116 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM | ||
| HCT15 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM | ||
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM | ||
| A10 cells | Growth inhibition assay | 48 h | Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM | ||
| HUVEC cells | Growth inhibition assay | 48 h | Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM | ||
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.001 μM | ||
| NCI-H522 cells | Growth inhibition assay | 48 h | Growth inhibition of human NCI-H522 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| MDA-MB-435 cells | Growth inhibition assay | 48 h | Growth inhibition of human MDA-MB-435 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| OVCAR3 | Growth inhibition assay | 48 h | Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| NCI/ADR-RES cells | Growth inhibition assay | 48 h | Growth inhibition of human NCI/ADR-RES cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| PC3 cells | Growth inhibition assay | 48 h | Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| DU145 cells | Growth inhibition assay | 48 h | Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| MDA-MB-231 cells | Growth inhibition assay | 48 h | Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| CEM cells | Cytotoxicity assay | 72 h | Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| HCT116 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| MDA-MB-435 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test, IC50=0.001 μM | ||
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| Hs578T cells | Growth inhibition assay | 48 h | Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM | ||
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | ||
| MDA-MB-468 cells | Cytotoxicity assay | 4 days | Cytotoxicity against human MDA-MB-468 cells assessed as cell viability after 4 days by MTS assay, IC50=0.0011 μM | ||
| MCF7 cells | Proliferation assay | 72 h | Antiproliferative activity in human MCF7 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00111 μM | ||
| NCI-H460 cells | Cytotoxicity assay | 72 h | Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test, IC50=0.0013 μM | ||
| OVCAR8 cells | Growth inhibition assay | 96 h | Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM | ||
| OVCAR8 cells | Cytotoxicity assay | 96 h | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM | ||
| NCI/ADR-RES cells | Cytotoxicity assay | 96 h | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition after 96 hrs by Giemsa staining-based light microscopy, IC50=0.0013 μM | ||
| HuTu 80 cells | Proliferation assay | 72 h | Antiproliferative activity in human HuTu 80 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00137 μM | ||
| SW620 cells | Proliferation assay | 72 h | Antiproliferative activity in human SW620 cells assessed as cell viability after 72 hrs by MTT assay, IC50=0.00152 μM | ||
| Molt4/C8 cells | Proliferation assay | 3 days | Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM | ||
| SKMEL-5 | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM | |||
| A-549 | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in A-549 lung carcinoma cell lines, ED50=1.20E-06 μM | |||
| MCF-7 | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in MCF-7 breast carcinoma cell lines, ED50=3.80E-06 μM | |||
| HT-29 | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in HT-29 colon adenocarcinoma cell lines, ED50=1.20E-06 μM | |||
| MLM melanoma cell | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM | |||
| M14 | Cytotoxicity assay | In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM | |||
| SK-OV3 | Cytotoxicity assay | In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM | |||
| HepG2 cells | Cytotoxicity assay | Cytotoxicity against human HepG2 cells, IC50=0.00014 μM | |||
| ZR-75-1 | Cytotoxicity assay | Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM | |||
| HeLa cell | Cytotoxicity assay | Cytotoxicity against HeLa cell line, IC50=0.0003 μM | |||
| HCT116 cell | Cytotoxicity assay | Cytotoxicity against HCT116 cell line, IC50=0.00035 μM | |||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM | |||
| SKOV3 cells | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM | |||
| HeLa cells | Cytotoxicity assay | Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM | |||
| DU145 cells | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM | |||
| DU145 cells | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM | |||
| HCT 116 | Growth inhibition assay | Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM | |||
| BNL 1ME A.7R.1 cells | Cytotoxicity assay | Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM | |||
| melanoma B16 cell | Growth inhibition assay | Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM | |||
| DU145 cells | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM | |||
| HaCaT cells | Proliferation assay | Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM | |||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM | |||
| SKOV3 cells | Growth inhibition assay | Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM | |||
| H460 | Cytotoxicity assay | Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM | |||
| H460 | Proliferation assay | Antiproliferative activity against human H460 cells, IC50=0.00124 μM | |||
| NCI/ADR-RES cells | Cytotoxicity assay | Cytotoxicity against human NCI/ADR-RES cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM | |||
| OVCAR8 cells | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM | |||
| K562 cells | Cytotoxicity assay | Cytotoxicity against human K562 cells, IC50=0.0014 μM | |||
| NCI/ADR (MDR) cells | Function assay | Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM | |||
| HUVEC | Proliferation assay | Antiproliferative activity against human HUVEC, IC50=0.0015 μM | |||
| KB cell | Proliferation assay | Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM | |||
| KB-VIN10 cell | Proliferation assay | Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM | |||
| Human SH-SY5Y neuroblastoma cells | Function assay | Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM | |||
| Molt4/C8 cells | Proliferation assay | Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM | |||
| ACHN cell | Proliferation assay | Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM | |||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產品描述 | Combretastatin A4 是一種以 microtubule 為靶點的試劑，其與β-微管蛋白結合，Kd 為 0.4 μM。Phase 3。 | ||
|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Combretastatin A4抑制MDA-MB-231，A549，Hela，HL-60，SF295，HCT-8，MDA-MB435，PC3M，OVCAR-8，NCI-H358M，和淋巴細胞的生長，IC50分別為2.8，3.8，0.9，2.1，6.2，5.3，7.9，4.7，0.37，8，和3.2 nM。[1] [2]1 μM Combretastatin A4抑制35%微管蛋白聚合，10 μM幾乎完全阻斷微管蛋白聚合。Combretastatin A4表現(xiàn)出高的相對結合能力，達到秋水仙堿結合力的78%。[1] | |||
|---|---|---|---|---|
| 激酶實驗 | 使用 LC-MS/MS 的競爭性結合試驗 | |||
| Colchicine (1.2 μ M)與微管蛋白(1.3 mg/mL)在培養(yǎng)緩沖液(80 mM PIPES，2.0 mM MgCl2，0.5 mM EGTA，pH 6.9)中于37℃下培養(yǎng)1小時。使用不同濃度(0.1? 125 μ M)的Combretastatin A4與原本結合微管蛋白的colchicine競爭。培育后，得到濾液。類似物抑制秋水仙堿結合的能力表示為不存在任何競爭物的對照組的百分比。 | ||||
| 細胞實驗 | 細胞系 | MDA-MB-231，A549，和 Hela 細胞 | ||
| 濃度 | ~3.8 nM | |||
| 孵育時間 | 72 h | |||
| 方法 | MDA-MB-231，A549，和HeLa細胞在DMEM培養(yǎng)基(115 units/mL 青霉素G，115 μg/mL 鏈霉素，和10%胎牛血清)中生長。細胞(5000 細胞/孔)接種于包含50 μL生長培養(yǎng)基的96孔板，培養(yǎng)24小時。移除培養(yǎng)基后，將100 μL包含不同濃度單個類似化合物的新鮮培養(yǎng)基加入到每個孔中，在37 ℃下培養(yǎng)72小時。培養(yǎng)24小時后，細胞中增補50 μL溶于DMSO(每個制劑中少于0.25%)的類似化合物。培養(yǎng)72小時后，加入20 μL刃天青培養(yǎng)2小時，然后在560 nm (激發(fā)波長)和590 nm (發(fā)射波長)下使用Victor微量滴定板熒光劑記錄熒光。對照組為用最大量DMSO (0.25%)處理的細胞，活性為100%，IC50定義為與對照組相比，抑制50%細胞增殖的化合物濃度。 | |||
| 體內研究(In Vivo) | ||
| 體內研究活性 | 在NT2和MDA-MB-231乳腺腫瘤模型中，Combretastatin A4 (100 mg/kg, i.p.)誘導脂質R1顯著減少，并通過電子順磁共振(EPR)血氧定量法測得pO2下降。[2] Combretastatin A4 (100 mg/kg, i.p.)顯著減少雄性NMRI小鼠的Ktrans。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 負荷 NT2 和 MDA-MB-231腫瘤的 FVB/N或裸的NMRI雄性小鼠 |
| Dosages | 100 mg/kg | |
| Administration | i.p. | |
|
化學信息&溶解度
| 分子量 | 316.35 | 分子式 | C18H20O5 |
| CAS號 | 117048-59-6 | SDF | Download Combretastatin A4 SDF |
| Smiles | COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 63 mg/mL ( (199.14 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 34 mg/mL (107.47 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | |||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
How to make solution for in vivo IP injection?
回答：
We've tested some vehicles for S7783 Combretastatin A4, and found it can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 30mg/ml clearly. When prepare the solution, please dissolve the compound in DMSO clearly first. The add PEG, after they mixed well, then dilute with water.
