Referencia número: HY-13270

ABT-751

(Synonyms: E7010)

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ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza: 98.74%
No. CAS: 141430-65-1
Fòrmula: C₁₈H₁₇N₃O₄S
Peso molecular:371.41

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ABT-751 Chemical Structure

No. CAS: 141430-65-1

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.17 μM Compound: 2, ABT-751	Cytotoxicity against human A2780 cells after 48 to 72 hrs by WAT-1 assay Cytotoxicity against human A2780 cells after 48 to 72 hrs by WAT-1 assay	[PMID: 21126027]
A549	GI₅₀	1.31 μM Compound: 2; E7010	Growth inhibition of human A549 cells after 48 hrs by SRB assay Growth inhibition of human A549 cells after 48 hrs by SRB assay	[PMID: 28400235]
A549	GI₅₀	1.31 μM Compound: E7010	Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 hrs by SRB assay	[PMID: 25468039]
A549	GI₅₀	1.8 μM Compound: 4; E7010	Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human A549 cells after 48 hrs by sulforhodamine B assay	[PMID: 27515320]
A549	GI₅₀	5.33 μM Compound: 4, ABT-751	Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 26241032]
A549	IC₅₀	1.31 μM Compound: 1, E7010	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 24835786]
A549	IC₅₀	1.31 μM Compound: ABT-751	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31546197]
A549	IC₅₀	1.376 μM Compound: ABT-751	Antiproliferative activity against human A549 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human A549 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
A549	IC₅₀	1.62 μM Compound: 11; ABT-751	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33479639]
ACHN	IC₅₀	2.13 μM Compound: 1, E7010	Cytotoxicity against human ACHN cells after 48 hrs by MTT assay Cytotoxicity against human ACHN cells after 48 hrs by MTT assay	[PMID: 24835786]
ASPC1	GI₅₀	4.11 μM Compound: 4, ABT-751	Cytotoxicity against human AsPC1 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human AsPC1 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 26241032]
BT-474	IC₅₀	8.39 μM Compound: ABT-751	Antiproliferative activity against human BT-474 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human BT-474 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
DU-145	GI₅₀	1.2 μM Compound: 4; E7010	Antiproliferative activity against human DU145 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human DU145 cells after 48 hrs by sulforhodamine B assay	[PMID: 27515320]
DU-145	GI₅₀	1.81 μM Compound: 2; E7010	Growth inhibition of human DU145 cells after 48 hrs by SRB assay Growth inhibition of human DU145 cells after 48 hrs by SRB assay	[PMID: 28400235]
DU-145	GI₅₀	1.81 μM Compound: E7010	Antiproliferative activity against human DU145 cells assessed as growth inhibition after 24 hrs by SRB assay Antiproliferative activity against human DU145 cells assessed as growth inhibition after 24 hrs by SRB assay	[PMID: 25468039]
DU-145	IC₅₀	1.31 μM Compound: ABT-751	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31546197]
DU-145	IC₅₀	1.81 μM Compound: 1, E7010	Cytotoxicity against human DU145 cells after 48 hrs by MTT assay Cytotoxicity against human DU145 cells after 48 hrs by MTT assay	[PMID: 24835786]
HCCLM3	IC₅₀	0.671 μM Compound: ABT-751	Antiproliferative activity against human HCCLM3 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human HCCLM3 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
HCT-116	IC₅₀	0.9 μM Compound: 2	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line	[PMID: 12383017]
HCT-116	IC₅₀	0.96 μM Compound: 2	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 -C1cell line Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 -C1cell line	[PMID: 12383017]
HCT-15	IC₅₀	340 nM Compound: E-7010	Antiproliferative activity against human colon carcinoma HCT-15 cell line(MDR(-)) Antiproliferative activity against human colon carcinoma HCT-15 cell line(MDR(-))	[PMID: 11425534]
HEK293	IC₅₀	1.31 μM Compound: ABT-751	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31546197]
HeLa	GI₅₀	4.8 μM Compound: 4; E7010	Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HeLa cells after 48 hrs by sulforhodamine B assay	[PMID: 27515320]
HeLa	IC₅₀	0.27 μM Compound: 2, ABT-751	Cytotoxicity against human HeLa cells after 48 to 72 hrs by WAT-1 assay Cytotoxicity against human HeLa cells after 48 to 72 hrs by WAT-1 assay	[PMID: 21126027]
HeLa	IC₅₀	0.355 μM Compound: 5; ABT-751	Growth inhibition of human HeLa cells incubated for 72 hrs by MTT assay Growth inhibition of human HeLa cells incubated for 72 hrs by MTT assay	[PMID: 27172319]
HeLa	IC₅₀	2.18 μM Compound: 11; ABT-751	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 33479639]
HeLa	IC₅₀	388 nM Compound: ABT-751	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by XTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by XTT assay	[PMID: 33328100]
Hep 3B2	GI₅₀	0.84 μM Compound: 4, ABT-751	Cytotoxicity against human Hep3B cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human Hep3B cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 26241032]
HepG2	GI₅₀	2.8 μM Compound: 4; E7010	Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay	[PMID: 27515320]
HepG2	IC₅₀	0.447 μM Compound: 5; ABT-751	Growth inhibition of human HepG2 cells incubated for 72 hrs by MTT assay Growth inhibition of human HepG2 cells incubated for 72 hrs by MTT assay	[PMID: 27172319]
HL-60	IC₅₀	0.2 μM Compound: 2; E7010	Cytotoxicity against human HL60 cells assessed as inhibition of cell growth after 3 days by MTT assay Cytotoxicity against human HL60 cells assessed as inhibition of cell growth after 3 days by MTT assay	[PMID: 27397495]
HL-60	IC₅₀	0.34 μM Compound: E7010	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	[PMID: 17276056]
HT-29	IC₅₀	0.21 μM Compound: 1; ABT-751	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 27538123]
HT-29	IC₅₀	0.21 μM Compound: E-7010	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23202849]
HT-29	IC₅₀	1.31 μM Compound: ABT-751	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31546197]
HT-29	IC₅₀	1.62 μM Compound: 1, E7010	Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay	[PMID: 24835786]
HT-29	IC₅₀	338.7 nM Compound: 5, ABT751	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay	[PMID: 24106982]
HT-29	IC₅₀	514 nM Compound: ABT-751	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by XTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by XTT assay	[PMID: 33328100]
HUVEC	IC₅₀	9.2 μM Compound: ABT-751	Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTS assay Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 24 hrs by MTS assay	[PMID: 33360794]
Jurkat	IC₅₀	0.16 μM Compound: 2, ABT-751	Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis	[PMID: 21126027]
KB	GI₅₀	0.801 μM Compound: 12; ABT-751, E7010	Antiproliferative activity against human KB cells incubated for 48 hrs by SRB assay Antiproliferative activity against human KB cells incubated for 48 hrs by SRB assay	[PMID: 32171161]
KB	IC₅₀	0.29 μg/mL Compound: E7010	In vitro antiproliferative activity (4 ug/mL) was measured against KB cancer cell line using MTT colorimetric assay In vitro antiproliferative activity (4 ug/mL) was measured against KB cancer cell line using MTT colorimetric assay	[PMID: 10866386]
KB	IC₅₀	0.29 μg/mL Compound: 5	In vitro inhibitory activity against KB (human carcinoma of the nasopharynx) cell proliferation. In vitro inhibitory activity against KB (human carcinoma of the nasopharynx) cell proliferation.	[PMID: 1619621]
KB	IC₅₀	0.29 μg/mL Compound: E7010	Antiproliferative activity against KB human nasopharynx carcinoma in vitro Antiproliferative activity against KB human nasopharynx carcinoma in vitro	[PMID: 10508428]
KB	IC₅₀	250 nM Compound: 1; ABT751	Growth inhibition of human KB cells after 48 hrs by SRB assay Growth inhibition of human KB cells after 48 hrs by SRB assay	[PMID: 30476825]
KB	IC₅₀	251.3 nM Compound: 5, ABT751	Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay	[PMID: 24106982]
MC-38	IC₅₀	0.38 μg/mL Compound: E7010	In vitro antiproliferative activity (4 ug/mL) was measured against colon 38 cancer cell line using MTT colorimetric assay In vitro antiproliferative activity (4 ug/mL) was measured against colon 38 cancer cell line using MTT colorimetric assay	[PMID: 10866386]
MC-38	IC₅₀	0.38 μg/mL Compound: 5	In vitro inhibitory activity against colon 38 cell proliferation In vitro inhibitory activity against colon 38 cell proliferation	[PMID: 1619621]
MC-38	IC₅₀	0.38 μg/mL Compound: E7010	In vitro antiproliferative activity against colon 38 murine adenocarcinoma In vitro antiproliferative activity against colon 38 murine adenocarcinoma	[PMID: 10508428]
MCF7	GI₅₀	1.25 μM Compound: E7010	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by SRB assay	[PMID: 25468039]
MCF7	GI₅₀	1.53 μM Compound: 2; E7010	Growth inhibition of human MCF7 cells after 48 hrs by SRB assay Growth inhibition of human MCF7 cells after 48 hrs by SRB assay	[PMID: 28400235]
MCF7	IC₅₀	1.25 μM Compound: 1, E7010	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24835786]
MCF7	IC₅₀	3.79 μM Compound: 5; ABT-751	Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay Growth inhibition of human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 27172319]
MKN-45	IC₅₀	166 nM Compound: 5, ABT751	Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay	[PMID: 24106982]
MKN-45	IC₅₀	170 nM Compound: 1; ABT751	Growth inhibition of human MKN45 cells after 48 hrs by SRB assay Growth inhibition of human MKN45 cells after 48 hrs by SRB assay	[PMID: 30476825]
MRC5	GI₅₀	>100 μM Compound: 2; E7010	Growth inhibition of human MRC5 cells after 48 hrs by SRB assay Growth inhibition of human MRC5 cells after 48 hrs by SRB assay	[PMID: 28400235]
NCI/ADR-RES	IC₅₀	0.29 μM Compound: 2, ABT-751	Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay	[PMID: 21126027]
NCI-H460	IC₅₀	2.036 μM Compound: ABT-751	Antiproliferative activity against human NCI-H460 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human NCI-H460 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
NCI-H460	IC₅₀	217.7 nM Compound: 5, ABT751	Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay	[PMID: 24106982]
NCI-H460	IC₅₀	350 nM Compound: E-7010	Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+)) Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+))	[PMID: 11425534]
NSCLC	IC₅₀	1.5 μM Compound: ABT-751; E 7010	Anticancer activity against human NSCLC cells Anticancer activity against human NSCLC cells	[PMID: 32324396]
P338	IC₅₀	0.16 μM Compound: 2; E7010	Cytotoxicity against mouse P338 cells assessed as inhibition of cell growth after 3 days by MTT assay Cytotoxicity against mouse P338 cells assessed as inhibition of cell growth after 3 days by MTT assay	[PMID: 27397495]
P388	IC₅₀	0.19 μM Compound: 2	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line	[PMID: 12383017]
P388	IC₅₀	0.32 μg/mL Compound: E7010	In vitro antiproliferative activity (4 ug/mL) was measured against P388 cancer cell line using MTT colorimetric assay In vitro antiproliferative activity (4 ug/mL) was measured against P388 cancer cell line using MTT colorimetric assay	[PMID: 10866386]
P388	IC₅₀	0.32 μg/mL Compound: E7010	Antiproliferative activity against P388 murine leukemia in vitro Antiproliferative activity against P388 murine leukemia in vitro	[PMID: 10508428]
P388	IC₅₀	15 μM Compound: 2	Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388/4.0 r-M cell line	[PMID: 12383017]
PANC-1	IC₅₀	0.837 μM Compound: ABT-751	Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human PANC-1 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
PC-3	GI₅₀	0.62 μM Compound: 4, ABT-751	Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 26241032]
PC-3	IC₅₀	0.46 μM Compound: 5; ABT-751	Growth inhibition of human PC3 cells incubated for 72 hrs by MTT assay Growth inhibition of human PC3 cells incubated for 72 hrs by MTT assay	[PMID: 27172319]
PLC-PRF-5	IC₅₀	0.792 μM Compound: ABT-751	Antiproliferative activity against human PLC-PRF-5 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human PLC-PRF-5 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
RKO	IC₅₀	0.633 μM Compound: ABT-751	Antiproliferative activity against human RKO cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human RKO cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
SGC-7901	IC₅₀	0.738 μM Compound: ABT-751	Antiproliferative activity against human SGC-7901 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human SGC-7901 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
SK-BR-3	IC₅₀	0.143 μM Compound: ABT-751	Antiproliferative activity against human SK-BR-3 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human SK-BR-3 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
SK-BR-3	IC₅₀	0.74 μM Compound: ABT-751	Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay	[PMID: 22850214]
SW480	IC₅₀	3.421 μM Compound: ABT-751	Antiproliferative activity against human SW480 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human SW480 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]
SW-620	IC₅₀	0.19 μM Compound: 2, ABT-751	Cytotoxicity against human SW620 cells after 48 to 72 hrs by WAT-1 assay Cytotoxicity against human SW620 cells after 48 to 72 hrs by WAT-1 assay	[PMID: 21126027]
SW-620	IC₅₀	2.787 μM Compound: ABT-751	Antiproliferative activity against human SW-620 cells assessed as cell viability measured after 72 hrs by MTS method Antiproliferative activity against human SW-620 cells assessed as cell viability measured after 72 hrs by MTS method	[PMID: 33360794]

In Vitro

ABT-751 (2 μM; 4, 8, 24h) can disrupt mitosis, disrupt mitochondrial membrane potential, induce ROS generation and DNA damage in hepatocellular carcinoma-derived Hep-3B cells ^[6].
ABT-751 (2 μM; 4, 8, 24h) can cause DNA damage in Hep-3B cells, inhibit cell proliferation and induce G2/M cell cycle arrest ^[6].
ABT-751 (2 μM; 4, 8, 24h) induces autophagy in TP53-deficient Hep-3B cells by inhibiting the AKT/MTOR signaling pathway, and induces apoptosis through Caspase-dependent, exogenous, and endogenous pathways. Exogenous expression of TP53 gene further increased the autophagy and apoptosis of these cells induced by ABT-751 [6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Line:
Concentration:
Incubation Time:
Result:

In Vivo

ABT-751 (100 mg/kg/day, Oral gavage (p.o.), 5 days on, 5 days off x2, 21 days) has a significant inhibitory effect in neuroblastoma models and can induce significant reduction or regression of tumor volume in rhabdomyosarcoma and nephroblastoma models. ABT-751 has synergistic effect on Vincristine and Paclitaxel (HY-B0015)^[7].
ABT-751 (100 mg/kg/day, Oral gavage (p.o.), 5 days on, 5 days off x2) has a synergistic effect on Docetaxel (HY-B0011) in prostate, NSCLC, and breast tumor xenografts in mice. Improve the inhibitory effect on tumor^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

xenograft models of neuroblastoma, osteosarcoma, Ewing sarcoma rhabdomyosarcoma, medulloblastoma and eight kidney cancer lines (six Wilms tumors, two rhabdoid)^[7]
Dosage:

100 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Had obvious inhibitory effect in neuroblastoma model.
Induced significant reduction or regression of tumor volume in rhabdomyosarcoma and nephroblastoma models.
Had a synergistic effect on vincristine or Paclitaxel (HY-B0015).

Animal Model:

PC-3 prostate, Calu-6 NSCLC, and breast MDA-MB-468 tumor xenografts in mice^[7]
Dosage:

75, 100 mg/kg
Administration:

Oral gavage (p.o.)
Result:

Had a synergistic effect with Docetaxel and improves the inhibitory effect on tumors.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 141430-65-1
Appearance Solid
Peso molecular 371.41
Fòrmula C₁₈H₁₇N₃O₄S
SMILES

COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O
Synonyms

E7010
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (269.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6924 mL

13.4622 mL

26.9244 mL

5 mM

0.5385 mL

2.6924 mL

5.3849 mL

10 mM

0.2692 mL

1.3462 mL

2.6924 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Huang SM et al.,Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling., Nature. 2009 Oct 1;461(7264):614-20. [Content Brief]

[2]. Elizabeth Fox et al. A Phase I Study of ABT-751, an Orally Bioavailable Tubulin Inhibitor, Administered Daily for 21 Days Every 28 Days in Pediatric Patients with Solid Tumors Clin Cancer Res February 15, 2008 14; 1111

[3]. Aggarwal C, et al. Antiangiogenic agents in the management of non-small cell lung cancer: where do we stand now and where are we headed?,Cancer Biol Ther. 2012 Mar;13(5):247-63. [Content Brief]

[4]. Silver M, Rusk A, Phillips B, Beck E, Jankowski M, Philibert J, Hahn K, Hershey E, McKeegan E, Bauch J, Krivoshik A, Khanna C.,Evaluation of the oral antimitotic agent (ABT-751) in dogs with lymphoma.,J Vet Intern Med. 2012 Mar-Apr;26(2):349-54. doi: 10.1111/j.1939-1676.2012.00892.x. Epub 2012 Feb 28. [Content Brief]

[5]. Gaynon PS, Harned TM; for the Therapeutic Advances in Childhood LeukemiaLymphoma (TACL) Consortium. [Content Brief]

[6]. Morton CL, et al. Evaluation of ABT-751 against childhood cancer models in vivo. Invest New Drugs. 2007;25(4):285-295. [Content Brief]

[7]. David Frost, et al. ABT-751, an oral antimitotic, shows additive and synergistic activity with docetaxel in preclinical models. Cancer Res 1 May 2007; 67 (9_Supplement): 1426.

[8]. Yoshimatsu K, et al. Mechanism of action of E7010, an orally active sulfonamide antitumor agent: inhibition of mitosis by binding to the colchicine site of tubulin. Cancer Res. 1997;57(15):3208-3213. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6924 mL	13.4622 mL	26.9244 mL	67.3111 mL
	5 mM	0.5385 mL	2.6924 mL	5.3849 mL	13.4622 mL
	10 mM	0.2692 mL	1.3462 mL	2.6924 mL	6.7311 mL
	15 mM	0.1795 mL	0.8975 mL	1.7950 mL	4.4874 mL
	20 mM	0.1346 mL	0.6731 mL	1.3462 mL	3.3656 mL
	25 mM	0.1077 mL	0.5385 mL	1.0770 mL	2.6924 mL
	30 mM	0.0897 mL	0.4487 mL	0.8975 mL	2.2437 mL
	40 mM	0.0673 mL	0.3366 mL	0.6731 mL	1.6828 mL
	50 mM	0.0538 mL	0.2692 mL	0.5385 mL	1.3462 mL
	60 mM	0.0449 mL	0.2244 mL	0.4487 mL	1.1219 mL
	80 mM	0.0337 mL	0.1683 mL	0.3366 mL	0.8414 mL
	100 mM	0.0269 mL	0.1346 mL	0.2692 mL	0.6731 mL

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ABT-751

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ABT-751

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Targeted Diversity Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Actividad biológica

Chemical Information

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

ABT-751 Related Classifications

HY-13270 Related Classifications