Home Cytoskeletal Signaling Microtubule Associated inhibitor Combretastatin A4 For research use only.

Combretastatin A4

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

Combretastatin A4 Chemical Structure

Combretastatin A4 Chemical Structure

CAS No. 117048-59-6

Purity & Quality Control

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

Combretastatin A4 Related Products

Signaling Pathway

Microtubule Associated Signaling Pathways

Microtubule Associated Signaling Pathway

Cell Data

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 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
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
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
KBV1 cells Cytotoxicity assay 72 h Cytotoxicity against human vinblastine-resistant KBV1 cells after 72 hrs by MTT assay, IC50=0.0004 μM 20731355
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
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
HCT 116 Growth inhibition assay Concentration which produces 50% inhibition of growth of human colon tumor HCT 116, IC50=0.0009 μM 11714613
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by resazurin based fluorescence assay, IC50=0.0009 μM 24669888
BNL 1ME A.7R.1 cells Cytotoxicity assay Cytotoxicity against mouse BNL 1ME A.7R.1 cells, IC50=0.0009 μM 25785605
Calu6 Proliferation assay 48 h Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry, IC50=0.00094 μM 21774499
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
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
HaCaT cells Proliferation assay Antiproliferative activity against human HaCaT cells assessed as cell viability by MTT assay, IC50=0.001 μM 23063401
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
HT-29 Growth inhibition assay Growth inhibition of human HT-29 cells by MTT assay, IC50=0.001 μM 25689111
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
SKOV3 cells Growth inhibition assay Growth inhibition of human SKOV3 cells by MTT assay, IC50=0.001 μM 25689111
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
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-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
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 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
OVCAR8 cells Cytotoxicity assay Cytotoxicity against human OVCAR8 cells assessed as growth inhibition by trypan blue exclusion assay, IC50=0.0013 μM 23214452
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
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
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 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
Molt4/C8 cells Proliferation assay 3 days Antiproliferative effect against human Molt4/C8 cells after 3 days, IC50=0.0016 μM 17419607
Click to View More Cell Line Experimental Data

Biological Activity

Description Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3.
Targets
β-tubulin [1]
0.4 μM(Kd)
In vitro
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] [2] 1 μM Combretastatin A4 inhibits tubulin polymerization by 35%, and 10 μM nearly completely blocks tubulin polymerization. Combretastatin A4 demonstrates great relative binding capacity, reaching 78% of colchicine binding.[1]
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 Combretastatin A4 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.
Cell Research Cell lines MDA-MB-231, A549, and Hela cells
Concentrations ~3.8 nM
Incubation Time 72 h
Method MDA-MB-231, A549, and HeLa cells are grown in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Cells are seeded in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, 100 μL of fresh medium containing individual analogue compounds at different concentrations is added to each well and incubated at 37 ℃ for 72 h. After 24 h of culture, the cells are supplemented with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, 20 μL of resazurin is added for 2 h before recording fluorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate fluorimeter. The IC50 is defined as the compound concentration required to inhibit cell proliferation by 50% in comparison with cells treated with the maximum amount of DMSO (0.25%) and considered as 100% viability.
In Vivo
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.[2] Combretastatin A4 (100 mg/kg, i.p.) significant decreases the Ktrans in male NMRI mice.[3]
Animal Research Animal Models FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors
Dosages 100 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 316.35 Formula

C18H20O5
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (199.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

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

Answer:
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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