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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(diǎn)的試劑，其與β-微管蛋白結(jié)合，Kd 為 0.4 μM。Phase 3。

Combretastatin A4 Chemical Structure

Combretastatin A4 Chemical Structure

CAS: 117048-59-6

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mg 811.66 現(xiàn)貨
50mg 3258.32 現(xiàn)貨
200mg 8166.98 現(xiàn)貨
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產(chǎn)品質(zhì)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(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

Microtubule Associated Signaling Pathways

Microtubule Associated信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Combretastatin A4 是一種以 microtubule 為靶點(diǎn)的試劑，其與β-微管蛋白結(jié)合，Kd 為 0.4 μM。Phase 3。
靶點(diǎn)
β-tubulin [1]
0.4 μM(Kd)
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(xì)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(duì)結(jié)合能力，達(dá)到秋水仙堿結(jié)合力的78%。[1]
激酶實(shí)驗(yàn) 使用 LC-MS/MS 的競爭性結(jié)合試驗(yàn)
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(shí)。使用不同濃度(0.1? 125 μ M)的Combretastatin A4與原本結(jié)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(jié)合的能力表示為不存在任何競爭物的對(duì)照組的百分比。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MDA-MB-231，A549，和 Hela 細(xì)胞
濃度 ~3.8 nM
孵育時(shí)間 72 h
方法 MDA-MB-231，A549，和HeLa細(xì)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(xì)胞(5000 細(xì)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(shí)。移除培養(yǎng)基后，將100 μL包含不同濃度單個(gè)類似化合物的新鮮培養(yǎng)基加入到每個(gè)孔中，在37 ℃下培養(yǎng)72小時(shí)。培養(yǎng)24小時(shí)后，細(xì)胞中增補(bǔ)50 μL溶于DMSO(每個(gè)制劑中少于0.25%)的類似化合物。培養(yǎng)72小時(shí)后，加入20 μL刃天青培養(yǎng)2小時(shí)，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(duì)照組為用最大量DMSO (0.25%)處理的細(xì)胞，活性為100%，IC50定義為與對(duì)照組相比，抑制50%細(xì)胞增殖的化合物濃度。
體內(nèi)研究(In Vivo)
體內(nèi)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(dǎo)脂質(zhì)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(dòng)物實(shí)驗(yàn) Animal Models 負(fù)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(xué)信息&溶解度

分子量 316.35 分子式

C18H20O5
CAS號(hào) 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(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 63 mg/mL ( (199.14 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 34 mg/mL (107.47 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)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(qǐng)先聯(lián)系Selleck）；

體內(nèi)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(nèi)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(jìn)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.

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