AVE-8063
Based on 1 Customer Validation
AVE-8063 (AC-7739 free base) is an aminocombretastatin. AVE-8063 shows potent antitubulin activity and cytotoxicity. AVE-8063 can be used in the research of leukemia and breast cancer.
For research use only. We do not sell to patients.
- Purity: 97.04%
- CAS No.: 162705-07-9
- Formula: C18H21NO4
- Molecular Weight:315.37
-
Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 3LL cell line | IC50 |
12 nM
Compound: 67
|
Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 10 mg/kg, ip qd for 4 days
Antitumor activity against mouse 3LL cells transplanted in to BALB/c mouse assessed as tumor growth inhibition at 10 mg/kg, ip qd for 4 days
|
[PMID: 20690624] |
| A549 | IC50 |
117 nM
Compound: AmCA-4
|
Antiproliferative activity against human A549 cells after 2 days by MTT assay
Antiproliferative activity against human A549 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| A549 | IC50 |
117 nM
Compound: AmCA-4
|
Antiproliferative activity against human A549 cells by MTT assay
Antiproliferative activity against human A549 cells by MTT assay
|
[PMID: 30502686] |
| A549 | IC50 |
51.2 nM
Compound: 15
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| BJ | IC50 |
87.3 nM
Compound: 15
|
Cytotoxicity against human BJ cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human BJ cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| BXPC-3 | GI50 |
0.43 ng/mL
Compound: 8f
|
Growth inhibition against human pancreas carcinoma cell line (BxPC-3)
Growth inhibition against human pancreas carcinoma cell line (BxPC-3)
|
[PMID: 15943482] |
| CCRF-CEM | IC50 |
51.2 nM
Compound: 15
|
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| CEM-DNR | IC50 |
15.7 nM
Compound: 15
|
Cytotoxicity against human CEM/DNR cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human CEM/DNR cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| Colon 26 | IC50 |
2.8 nM
Compound: 5
|
Antiproliferative activity against mouse Colon 26 cells assessed as inhibition of cell growth
Antiproliferative activity against mouse Colon 26 cells assessed as inhibition of cell growth
|
[PMID: 23454513] |
| Colon 26 | IC50 |
5.1 nM
Compound: 21a
|
Growth inhibition of colon 26 adenocarcinoma cells by 50 %.
Growth inhibition of colon 26 adenocarcinoma cells by 50 %.
|
[PMID: 9685242] |
| DU-145 | GI50 |
0.33 ng/mL
Compound: 8f
|
Growth inhibition against human prostate cell line (DU-145)
Growth inhibition against human prostate cell line (DU-145)
|
[PMID: 15943482] |
| DU-145 | GI50 |
0.96 ng/mL
Compound: 3'-NH2-CA4
|
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells after 48 hrs by SRB assay
|
[PMID: 18710804] |
| DU-145 | GI50 |
3.3 nM
Compound: 3' CA4-amine
|
Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by SRB assay
|
[PMID: 26852340] |
| FaDu | GI50 |
0.53 ng/mL
Compound: 8f
|
Growth inhibition against human pharynx FADU cell line
Growth inhibition against human pharynx FADU cell line
|
[PMID: 15943482] |
| HCT-116 | IC50 |
269 nM
Compound: 67
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 20690624] |
| HCT-116 | IC50 |
3.17 nM
Compound: 15
|
Cytotoxicity against p53 deficient human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against p53 deficient human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| HCT-116 | IC50 |
3.18 nM
Compound: 15
|
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| HCT-15 | IC50 |
45.2 nM
Compound: 67
|
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT15 cells after 72 hrs by MTT assay
|
[PMID: 20690624] |
| HCT-15 | IC50 |
6.5 μM
Compound: 67
|
Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
Inhibition of tubulin polymerization in multidrug-resistant human HCT15 cells after 1 hr
|
[PMID: 20690624] |
| HEK293 | IC50 |
7.1 nM
Compound: AmCA-4
|
Antiproliferative activity against HEK293 cells after 2 days by MTT assay
Antiproliferative activity against HEK293 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| HEK293 | IC50 |
7.1 nM
Compound: AmCA-4
|
Antiproliferative activity against HEK293 cells by MTT assay
Antiproliferative activity against HEK293 cells by MTT assay
|
[PMID: 30502686] |
| HeLa | CC50 |
1.47 nM
Compound: 3
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay
|
[PMID: 31413794] |
| HeLa | IC50 |
0.403 μM
Compound: 3, AVE8063
|
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity against human HeLa cells after 24 hrs by MTT assay
|
[PMID: 23369687] |
| HeLa | IC50 |
0.53 nM
Compound: 19
|
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
|
[PMID: 19879758] |
| HeLa | IC50 |
2.6 nM
Compound: AmCA-4
|
Antiproliferative activity against human HeLa cells after 2 days by MTT assay
Antiproliferative activity against human HeLa cells after 2 days by MTT assay
|
[PMID: 29432949] |
| HeLa | IC50 |
2.6 nM
Compound: AmCA-4
|
Antiproliferative activity against human HeLa cells by MTT assay
Antiproliferative activity against human HeLa cells by MTT assay
|
[PMID: 30502686] |
| HepG2 | IC50 |
0.028 μM
Compound: 3, AVE8063
|
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
|
[PMID: 23369687] |
| HL-60 | IC50 |
0.012 μM
Compound: AVE-8063
|
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 20850313] |
| HL-60 | IC50 |
12 nM
Compound: 67
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 20690624] |
| HL-60 | IC50 |
4.5 nM
Compound: AmCA-4
|
Antiproliferative activity against human HL60 cells after 2 days by MTT assay
Antiproliferative activity against human HL60 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| HL-60 | IC50 |
4.5 nM
Compound: AmCA-4
|
Antiproliferative activity against human HL60 cells by MTT assay
Antiproliferative activity against human HL60 cells by MTT assay
|
[PMID: 30502686] |
| HMEC-1 | IC50 |
0.012 μM
Compound: AmCA-4
|
Antiangiogenic activity against HMEC1 cells after 20 hrs by tube formation assay
Antiangiogenic activity against HMEC1 cells after 20 hrs by tube formation assay
|
[PMID: 30502686] |
| HMEC-1 | IC50 |
12 nM
Compound: AmCA-4
|
Antiproliferative activity against HMEC1 cells after 2 days by MTT assay
Antiproliferative activity against HMEC1 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| HMEC-1 | IC50 |
12 nM
Compound: AmCA-4
|
Antiproliferative activity against HMEC1 cells by MTT assay
Antiproliferative activity against HMEC1 cells by MTT assay
|
[PMID: 30502686] |
| HT-29 | IC50 |
22 nM
Compound: AmCA-4
|
Antiproliferative activity against human HT-29 cells after 2 days by MTT assay
Antiproliferative activity against human HT-29 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| HT-29 | IC50 |
22 nM
Compound: AmCA-4
|
Antiproliferative activity against human HT-29 cells by MTT assay
Antiproliferative activity against human HT-29 cells by MTT assay
|
[PMID: 30502686] |
| HT-29 | IC50 |
5 nM
Compound: 3b, ST-3100
|
Cytotoxic activity against human HT29 cells after 72 hrs by sulforhodamine B test
Cytotoxic activity against human HT29 cells after 72 hrs by sulforhodamine B test
|
[PMID: 18396857] |
| HT-29 | IC50 |
5 nM
Compound: 9, AVE-8063
|
Antiproliferative activity against human HT29 cell line by methylene blue dye assay
Antiproliferative activity against human HT29 cell line by methylene blue dye assay
|
[PMID: 17034147] |
| HT-29 | IC50 |
7.9 nM
Compound: AVE-8063
|
In vitro cytotoxic activity against human HT-29 cell line of colorectal carcinoma
In vitro cytotoxic activity against human HT-29 cell line of colorectal carcinoma
|
[PMID: 15139768] |
| Huh-7 | CC50 |
>100 μM
Compound: 3
|
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 24 hrs by cell titer blue assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 24 hrs by cell titer blue assay
|
[PMID: 31413794] |
| Huh-7 | CC50 |
3.93 nM
Compound: 3
|
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability measured after 72 hrs by cell titer blue assay
|
[PMID: 31413794] |
| HUVEC | IC50 |
11.3 nM
Compound: 15
|
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| K562 | IC50 |
0.12 μM
Compound: 3, AVE8063
|
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
Cytotoxicity against human K562 cells after 24 hrs by MTT assay
|
[PMID: 23369687] |
| K562 | IC50 |
15.7 nM
Compound: 15
|
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
| KB | IC50 |
7 nM
Compound: 9, AVE-8063
|
Antiproliferative activity against human KB cell line by methylene blue dye assay
Antiproliferative activity against human KB cell line by methylene blue dye assay
|
[PMID: 17034147] |
| KB | IC50 |
8.2 nM
Compound: AVE-8063
|
In vitro cytotoxic activity against human KB cell line of epidermoid carcinoma
In vitro cytotoxic activity against human KB cell line of epidermoid carcinoma
|
[PMID: 15139768] |
| MCF7 | IC50 |
0.0035 μM
Compound: 19
|
Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
|
[PMID: 19879758] |
| MCF7 | IC50 |
8 nM
Compound: AmCA-4
|
Antiproliferative activity against human MCF7 cells after 2 days by MTT assay
Antiproliferative activity against human MCF7 cells after 2 days by MTT assay
|
[PMID: 29432949] |
| MCF7 | IC50 |
8 nM
Compound: AmCA-4
|
Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
|
[PMID: 30502686] |
| MDA-MB-231 | IC50 |
12 nM
Compound: AmCA-4
|
Antiproliferative activity against human MDA-MB-231 cells after 3 days by coulter counting method
Antiproliferative activity against human MDA-MB-231 cells after 3 days by coulter counting method
|
[PMID: 29432949] |
| MDA-MB-231 | IC50 |
45 nM
Compound: AVE-8063
|
Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against P-gp expressing multidrug-resistant human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 20850313] |
| MKN-45 | IC50 |
5.1 nM
Compound: 9, AVE-8063
|
Antiproliferative activity against human MKN45 cell line by methylene blue dye assay
Antiproliferative activity against human MKN45 cell line by methylene blue dye assay
|
[PMID: 17034147] |
| NCI-H460 | GI50 |
0.33 ng/mL
Compound: 8f
|
Growth inhibition against human lung-NSC NCI-H460 cell line
Growth inhibition against human lung-NSC NCI-H460 cell line
|
[PMID: 15943482] |
| NCI-H460 | GI50 |
0.68 ng/mL
Compound: 3'-NH2-CA4
|
Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells after 48 hrs by SRB assay
|
[PMID: 18710804] |
| NCI-H460 | GI50 |
4.49 nM
Compound: 3' CA4-amine
|
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 48 hrs by SRB assay
|
[PMID: 26852340] |
| NCI-H460 | IC50 |
4.9 nM
Compound: 3b, ST-3100
|
Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test
Cytotoxic activity against human NCI-H460 cells after 72 hrs by sulforhodamine B test
|
[PMID: 18396857] |
| NCI-H460 | IC50 |
9 nM
Compound: 9, AVE-8063
|
Antiproliferative activity against human H460 cell line by methylene blue dye assay
Antiproliferative activity against human H460 cell line by methylene blue dye assay
|
[PMID: 17034147] |
| P388 | ED50 |
>0.01 μg/mL
Compound: 8f
|
Effective dose against murine P388 leukemia cell line
Effective dose against murine P388 leukemia cell line
|
[PMID: 15943482] |
| SK-N-SH | GI50 |
0.23 ng/mL
Compound: 8f
|
Growth inhibition against human neuroblastoma cell line (SK-N-SH)
Growth inhibition against human neuroblastoma cell line (SK-N-SH)
|
[PMID: 15943482] |
| SK-OV-3 | GI50 |
4.45 nM
Compound: 3' CA4-amine
|
Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay
Cytotoxicity against human SKOV3 cells assessed as growth inhibition after 48 hrs by SRB assay
|
[PMID: 26852340] |
| SW-1736 | GI50 |
0.8 ng/mL
Compound: 8f
|
Growth inhibition against human thyroid cell line( SW 1736)
Growth inhibition against human thyroid cell line( SW 1736)
|
[PMID: 15943482] |
| TSGH | IC50 |
7.7 nM
Compound: AVE-8063
|
In vitro cytotoxic activity against human TSGH cell line of stomach carcinoma
In vitro cytotoxic activity against human TSGH cell line of stomach carcinoma
|
[PMID: 15139768] |
| TSGH 9201 | IC50 |
7 nM
Compound: 9, AVE-8063
|
Antiproliferative activity against human TSGH stomach carcinoma cell line by methylene blue dye assay
Antiproliferative activity against human TSGH stomach carcinoma cell line by methylene blue dye assay
|
[PMID: 17034147] |
| U2OS | IC50 |
6 nM
Compound: 15
|
Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
|
[PMID: 31401010] |
Chemical Information
-
CAS No. 162705-07-9
-
Appearance Liquid
-
Molecular Weight 315.37
-
Formula C18H21NO4
-
Color Yellow to brown
-
SMILES
O(C)C1=C(OC)C=C(/C=C\C2=CC(N)=C(OC)C=C2)C=C1OC
-
Synonyms
AC-7739 free base
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Purity & Documentation
-
Data Sheet (269 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
[1]. Kamal A, et al. Synthesis and biological evaluation of 1,2,3-triazole linked aminocombretastatin conjugates as mitochondrial mediated apoptosis inducers. Bioorg Med Chem. 2014 Oct 1;22(19):5155-67. [Content Brief]
[2]. Lee J, et al. Discovery of a potent tubulin polymerization inhibitor: synthesis and evaluation of water-soluble prodrugs of benzophenone analog. Bioorg Med Chem Lett. 2010 Nov 1;20(21):6327-30. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)