AVE-8063 (Synonyms: AC-7739 free base)

Cat. No.: HY-117867 Purity: 97.04%: Data Sheet
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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.

AVE-8063 Chemical Structure

CAS No. : 162705-07-9

Size	Stock	Quantity
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
250 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Description

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^[1]^[2].

Cellular Effect

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]

Molecular Weight

315.37

Formula

C₁₈H₂₁NO₄

CAS No.

162705-07-9

Appearance

Liquid

Color

Yellow to brown

SMILES

O(C)C1=C(OC)C=C(/C=C\C2=CC(N)=C(OC)C=C2)C=C1OC

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

Purity: 97.04%

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Data Sheet (269 KB) SDS (393 KB)

COA (251 KB) HNMR (221 KB) RP-HPLC (127 KB) LCMS (139 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]

AVE-8063 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AVE-8063162705-07-9AC-7739AVE8063AVE 8063AC7739AC 7739Microtubule/TubulinInhibitorinhibitorinhibit

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AVE-8063 (Synonyms: AC-7739 free base)

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AVE-8063 Related Classifications

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