Home Cytoskeletal Signaling Microtubule Associated inhibitor Combretastatin A4

research use only

Combretastatin A4 Microtubule Associated inhibitor

Cat.No.S7783

Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM. Phase 3.
Combretastatin A4 Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 316.35

Jump to

Quality Control

Batch: S778301 DMSO]63 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
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
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
KBV1 cells Cytotoxicity assay 72 h Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 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
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
HCT 116 Growth inhibition assay Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, 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
Calu6 Proliferation assay 48 h Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 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
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
HaCaT cells Proliferation assay Antiproliferative activity against human HaCaT cells assessed as cell viability 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
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells 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
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
SKOV3 cells Growth inhibition assay Growth inhibition of human SKOV3 cells 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
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-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
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 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
OVCAR8 cells Cytotoxicity assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, 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
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
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 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
Molt4/C8 cells Proliferation assay 3 days Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (199.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 316.35 Formula

C18H20O5

 Storage (From the date of receipt)
CAS No. 117048-59-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)O

Mechanism of Action

Targets/IC50/Ki
β-tubulin
0.4 μM(Kd)
In vitro
Combretastatin A4 inhibits the growth of MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M, and lymphocyte cells with IC50 of 2.8, 3.8, 0.9, 2.1, 6.2, 5.3, 7.9, 4.7, 0.37, 8, and 3.2 nM, respectively. 1 μM of this compound inhibits tubulin polymerization by 35%, and 10 μM nearly completely blocks tubulin polymerization. This chemical demonstrates great relative binding capacity, reaching 78% of colchicine binding.
Kinase Assay
Competitive binding assay using LC-MS/MS
Colchicine (1.2 μ M) is incubated with tubulin (1.3 mg/mL) in the incubation buffer (80 mM PIPES, 2.0 mM MgCl2, 0.5 mM EGTA, pH 6.9) at 37℃ for 1 h. Varying concentrations (0.1 − 125 μ M) of this compound are used to compete with colchicine originally bound to tubulin. After incubation, the filtrate is obtained. The ability of the analogue to inhibit the binding of colchicine is expressed as a percentage of control binding in the absence of any competitor.
In vivo
In NT2 and MDA-MB-231 mammary tumor model, administration of Combretastatin A4 (100 mg/kg, i.p.) induces a significant decrease in lipids R1 and a reduction in tumor pO2 measured by electron paramagnetic resonance (EPR) oximetry. This compound (100 mg/kg, i.p.) significant decreases the Ktrans in male NMRI mice.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
How to make solution for in vivo IP injection of it?

Answer:
We've tested some vehicles for this compound, and found it can be dissolved in 5% DMSO+50% PEG 300+ddH2O at 30mg/ml clearly. When prepare the solution, please dissolve it in DMSO clearly first. Then add PEG, after they mixed well, then dilute with water.

Signaling Pathway Map