Combretastatin A4
中文名称：康普立停 A4
Combretastatin A4 是一种以 microtubule 为靶点的试剂，其与β-微管蛋白结合，Kd 为 0.4 μM。Phase 3。
Combretastatin A4 Chemical Structure
CAS: 117048-59-6
产品质控
批次：
S778301
DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false
纯度：
99.87%
99.87
Combretastatin A4相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.0001 μM | 20731355 | |
| 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 | 18722127 | |
| KBV1 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM | 20731355 | |
| 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 | 22329561 | |
| NCIH460 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human NCIH460 cells after 48 hrs by SRB assay, GI50=0.0006 μM | 18303849 | |
| 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 | 21641700 | |
| 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 | 21955454 | |
| DU145 cells | Cytotoxicity assay | 48 h | Cytotoxicity against human DU145 cells after 48 hrs by SRB assay, GI50=0.0008 μM | 18303849 | |
| 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 | 25785605 | |
| HeLa cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM | 24669888 | |
| Calu6 | Proliferation assay | 48 h | Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM | 21774499 | |
| HCT116 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50=0.001 μM | 21112130 | |
| HCT15 cells | Proliferation assay | 72 h | Antiproliferative activity against human HCT15 cells after 72 hrs by MTS assay, IC50=0.001 μM | 21112130 | |
| 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 | 21663319 | |
| A10 cells | Growth inhibition assay | 48 h | Growth inhibition of rat A10 cells after 48 hrs by MTT assay, IC50=0.001 μM | 22044164 | |
| HUVEC cells | Growth inhibition assay | 48 h | Growth inhibition of HUVEC cells after 48 hrs by MTT assay, IC50=0.001 μM | 22044164 | |
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 22136312 | |
| 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 | 22578111 | |
| 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 | 22982122 | |
| 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 | 22982122 | |
| OVCAR3 | Growth inhibition assay | 48 h | Growth inhibition of human OVCAR3 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 | |
| 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 | 22982122 | |
| PC3 cells | Growth inhibition assay | 48 h | Growth inhibition of human PC3 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 | |
| DU145 cells | Growth inhibition assay | 48 h | Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 | |
| 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 | 22982122 | |
| CEM cells | Cytotoxicity assay | 72 h | Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50=0.001 μM | 22676247 | |
| HCT116 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.001 μM | 22676247 | |
| 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 | 22676247 | |
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 23117171 | |
| 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 | 25785605 | |
| HL60 cells | Proliferation assay | 72 h | Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 20420439 | |
| Hs578T cells | Growth inhibition assay | 48 h | Growth inhibition of human Hs578T cells after 48 hrs by SRB assay, GI50=0.001 μM | 22982122 | |
| HL60 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=0.001 μM | 23445496 | |
| 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 | 24210503 | |
| 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 | 22329561 | |
| 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 | 18396857 | |
| OVCAR8 cells | Growth inhibition assay | 96 h | Growth inhibition of human OVCAR8 cells overexpressing P-glycoprotein after 96 hrs, IC50=0.0013 μM | 22044164 | |
| 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 | 25025991 | |
| 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 | 25025991 | |
| 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 | 22329561 | |
| 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 | 22329561 | |
| Molt4/C8 cells | Proliferation assay | 3 days | Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM | 17419607 | |
| SKMEL-5 | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in SKMEL-5 melanoma cell lines, ED50=3.00E-08 μM | 1875350 | ||
| 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 | 1875350 | ||
| 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 | 1875350 | ||
| 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 | 1875350 | ||
| MLM melanoma cell | Growth inhibition assay | Cytotoxic concentration required to inhibit 50% cell growth in MLM melanoma cell lines, ED50=1.40E-06 μM | 1875350 | ||
| M14 | Cytotoxicity assay | In vitro cytotoxic activity was tested against human melanoma cancer (M14) cell line, GI50=0.0001 μM | 12729640 | ||
| SK-OV3 | Cytotoxicity assay | In vitro cytotoxic activity tested against human ovarian cancer (SK-OV3) cell line, GI50=0.0001 μM | 12729640 | ||
| HepG2 cells | Cytotoxicity assay | Cytotoxicity against human HepG2 cells, IC50=0.00014 μM | 17127061 | ||
| ZR-75-1 | Cytotoxicity assay | Cytotoxicity against ZR-75-1 cell line, IC50=0.00024 μM | 17249649 | ||
| HeLa cell | Cytotoxicity assay | Cytotoxicity against HeLa cell line, IC50=0.0003 μM | 17249649 | ||
| HCT116 cell | Cytotoxicity assay | Cytotoxicity against HCT116 cell line, IC50=0.00035 μM | 17249649 | ||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50=0.00042 μM | 24016002 | ||
| SKOV3 cells | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B assay, GI50=0.00042 μM | 23772309 | ||
| HeLa cells | Cytotoxicity assay | Cytotoxicity against human HeLa cells by MTT assay, IC50=0.00051 μM | 19879758 | ||
| DU145 cells | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.00054 μM | 24016002 | ||
| DU145 cells | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B assay, GI50=0.00054 μM | 23772309 | ||
| HCT 116 | Growth inhibition assay | Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM | 11714613 | ||
| BNL 1ME A.7R.1 cells | Cytotoxicity assay | Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM | 25785605 | ||
| melanoma B16 cell | Growth inhibition assay | Concentration which produces 50% inhibition of growth of murine melanoma B16 cell line, IC50=0.001 μM | 11714613 | ||
| DU145 cells | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50=0.001 μM | 20496923 | ||
| HaCaT cells | Proliferation assay | Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM | 23063401 | ||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM | 25689111 | ||
| SKOV3 cells | Growth inhibition assay | Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM | 25689111 | ||
| H460 | Cytotoxicity assay | Cytotoxicity against human H460 cells by sulforhodamine B test, IC50=0.0012 μM | 18783207 | ||
| H460 | Proliferation assay | Antiproliferative activity against human H460 cells, IC50=0.00124 μM | 16722633 | ||
| 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 | 23214452 | ||
| OVCAR8 cells | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM | 23214452 | ||
| K562 cells | Cytotoxicity assay | Cytotoxicity against human K562 cells, IC50=0.0014 μM | 19837594 | ||
| NCI/ADR (MDR) cells | Function assay | Cell cycle arrest in NCI/ADR (MDR) cells by accumulation at G2/M phase, IC50=0.0015 μM | 16377187 | ||
| HUVEC | Proliferation assay | Antiproliferative activity against human HUVEC, IC50=0.0015 μM | 16722633 | ||
| KB cell | Proliferation assay | Antiproliferative activity against human KB cell line by methylene blue dye assay, IC50=0.0015 μM | 17034147 | ||
| KB-VIN10 cell | Proliferation assay | Antiproliferative activity against human KB-VIN10 cell line by methylene blue dye assay, IC50=0.0015 μM | 17034147 | ||
| Human SH-SY5Y neuroblastoma cells | Function assay | Inhibitory concentration against Human SH-SY5Y neuroblastoma cells, IC50=0.0015 μM | 15963722 | ||
| Molt4/C8 cells | Proliferation assay | Antiproliferative activity against human Molt4/C8 cells, IC50=0.0016 μM | 17034150 | ||
| ACHN cell | Proliferation assay | Antiproliferative activity against drug resistant ACHN cell line expressing MDR1 by Alamar Blue assay, IC50=0.0016 μM | 17286393 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Combretastatin A4 是一种以 microtubule 为靶点的试剂，其与β-微管蛋白结合，Kd 为 0.4 μM。Phase 3。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | Combretastatin A4抑制MDA-MB-231，A549，Hela，HL-60，SF295，HCT-8，MDA-MB435，PC3M，OVCAR-8，NCI-H358M，和淋巴细胞的生长，IC50分别为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几乎完全阻断微管蛋白聚合。Combretastatin A4表现出高的相对结合能力，达到秋水仙碱结合力的78%。[1] | |||
|---|---|---|---|---|
| 激酶实验 | 使用 LC-MS/MS 的竞争性结合试验 | |||
| Colchicine (1.2 μ M)与微管蛋白(1.3 mg/mL)在培养缓冲液(80 mM PIPES，2.0 mM MgCl2，0.5 mM EGTA，pH 6.9)中于37℃下培养1小时。使用不同浓度(0.1− 125 μ M)的Combretastatin A4与原本结合微管蛋白的colchicine竞争。培育后，得到滤液。类似物抑制秋水仙碱结合的能力表示为不存在任何竞争物的对照组的百分比。 | ||||
| 细胞实验 | 细胞系 | MDA-MB-231，A549，和 Hela 细胞 | ||
| 浓度 | ~3.8 nM | |||
| 孵育时间 | 72 h | |||
| 方法 | MDA-MB-231，A549，和HeLa细胞在DMEM培养基(115 units/mL 青霉素G，115 μg/mL 链霉素，和10%胎牛血清)中生长。细胞(5000 细胞/孔)接种于包含50 μL生长培养基的96孔板，培养24小时。移除培养基后，将100 μL包含不同浓度单个类似化合物的新鲜培养基加入到每个孔中，在37 ℃下培养72小时。培养24小时后，细胞中增补50 μL溶于DMSO(每个制剂中少于0.25%)的类似化合物。培养72小时后，加入20 μL刃天青培养2小时，然后在560 nm (激发波长)和590 nm (发射波长)下使用Victor微量滴定板荧光剂记录荧光。对照组为用最大量DMSO (0.25%)处理的细胞，活性为100%，IC50定义为与对照组相比，抑制50%细胞增殖的化合物浓度。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在NT2和MDA-MB-231乳腺肿瘤模型中，Combretastatin A4 (100 mg/kg, i.p.)诱导脂质R1显著减少，并通过电子顺磁共振(EPR)血氧定量法测得pO2下降。[2] Combretastatin A4 (100 mg/kg, i.p.)显著减少雄性NMRI小鼠的Ktrans。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 负荷 NT2 和 MDA-MB-231肿瘤的 FVB/N或裸的NMRI雄性小鼠 |
| Dosages | 100 mg/kg | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 316.35 | 分子式 | C18H20O5 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 63 mg/mL ( (199.14 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 34 mg/mL (107.47 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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.
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