Home Cytoskeletal Signaling Microtubule Associated inhibitor ABT-751 (E7010) For research use only.

ABT-751 (E7010)

ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.

ABT-751 (E7010) Chemical Structure

ABT-751 (E7010) Chemical Structure

CAS: 141430-65-1

Selleck's ABT-751 (E7010) has been cited by 5 Publications

3 Customer Reviews

Purity & Quality Control

Batch: S116501 DMSO] 74 mg/mL] false] Ethanol] 12 mg/mL] false] Water] Insoluble] false Purity: 99.95%
99.95

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT-15 cell Proliferation assay Antiproliferative activity against human colon carcinoma HCT-15 cell line(MDR(-)), IC50=0.34 μM 11425534
HCT116-C9 cell Function assay Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in HCT116-C9 cell line, IC50=0.9 μM 12383017
NCI-H460 cell Proliferation assay Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+)), IC50=0.35 μM 11425534
P388 cell line Function assay 72 h Effective concentration to inhibit cell proliferation by 50% relative to untreated control cell after 72 hr of continuous exposure in P388 cell line， IC50=0.19 μM 12383017
P388/4.0 r-M cell line Function assay 72 h 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, IC50=15 μM 12383017
human HL60 cells Proliferation assay Antiproliferative activity against human HL60 cells, IC50=0.34 μM 17276056
HeLa cells Cytotoxicity assay 48-72 h Cytotoxicity against human HeLa cells after 48 to 72 hrs by WAT-1 assay, IC50=0.27 μM 21126027
MDR1 cells Cytotoxicity assay 48-72 h Cytotoxicity against human NCI-ADR-RES expressing MDR1 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.29 μM 21126027
Jurkat cells Function assay 24 h Cell cycle arrest in human Jurkat cells assessed as accumulation at G2/M phase after 24 hrs using propidium iodide staining by FACS analysis, IC50=0.16 μM 21126027
SW620 cells Cytotoxicity assay 48-72 h Cytotoxicity against human SW620 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.19 μM 21126027
A2780 cells Cytotoxicity assay 48-72 h Cytotoxicity against human A2780 cells after 48 to 72 hrs by WAT-1 assay, IC50=0.17 μM 21126027
HT-29 cells Proliferation assay 72 h Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.21 μM 23202849
HUVEC Function assay 100-1000 nM 4 h Induction of vascular disrupting activity in HUVEC assessed as VEGF-induced tube formation at 100 to 1000 nM after 4 hrs by microscopic analysis 24106982
H460 cells Cytotoxicity assay 72 h Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2177 μM 24106982
MKN45 cells Cytotoxicity assay 72 h Cytotoxicity against human MKN45 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.166 μM 24106982
HT-29 cells Cytotoxicity assay 72 h Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.3387 μM 24106982
human A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=1.31 μM 24835786
ACHN cells Cytotoxicity assay 48 h Cytotoxicity against human ACHN cells after 48 hrs by MTT assay, IC50=2.13 μM 24835786
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.25 μM 24835786
HT-29 cells Cytotoxicity assay 48 h Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=1.62 μM 24835786
A549 cells Proliferation assay 24 h Antiproliferative activity against human A549 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.31 μM 25468039
human MCF7 cells Proliferation assay 24 h Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.25 μM 25468039
KB-S15 cells Cytotoxicity assay 72 h Cytotoxicity against human KB-S15 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.206 μM 24106982
KB-7d cells Cytotoxicity assay 72 h Cytotoxicity against human KB-7d cells overexpressing MRP assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.205 μM 24106982
KB-VIN10 cells Cytotoxicity assay 72 h Cytotoxicity against human KB-VIN10 cells overexpressing P-gp170/MDR assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.227 μM 24106982
human PC3 cells Cytotoxicity assay 48 h Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.62 μM 26241032
human AsPC1 cells Cytotoxicity assay 48 h Cytotoxicity against human AsPC1 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=4.11 μM 26241032
human A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=5.33 μM 26241032
Hep3B cells Cytotoxicity assay 48 h Cytotoxicity against human Hep3B cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay, GI50=0.84 μM 26241032
KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells assessed as growth inhibition after 72 hrs by methylene blue staining-based assay, IC50=0.2513 μM 24106982
DU145 cells Proliferation assay 24 h Antiproliferative activity against human DU145 cells assessed as growth inhibition after 24 hrs by SRB assay, GI50=1.81 μM 25468039
DU145 cells Cytotoxicity assay 48 h Cytotoxicity against human DU145 cells after 48 hrs by MTT assay， GI50=1.81 μM 24835786
human SKBR3 cells Growth inhibition assay 48 h Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50=0.74 μM 22850214
Click to View More Cell Line Experimental Data

Biological Activity

Description ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules, not a substrate for the MDR transporter and is active against cell lines resistant to vincristine, doxorubicin, and cisplatin. Phase 1/2.
Features An orally bioavailable tubulin-binding and antimitotic sulfonamide.
Targets
Microtubules [1]
In vitro
In vitro In vitro, ABT-751 shows the selective cytotoxicity with IC50 of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. Furthermore, ABT-751 also exhibits a selective effect on dynamic microtubules and spares stable microtubules, accounting for the persistence of acetylated and detyrosinated α-tubulin positive polymerized tubules at the IC90 concentration of ABT-751. [1]
Cell Research Cell lines HOS, HTB-186 Daoy, TC-71, RD, SK-N-AS, SK-N-DZ, LD and KCNR cells
Concentrations 0 to 100 μM
Incubation Time 72 hours
Method Cells, in 1640 RPMI media with FBS, are plated in triplicate onto 96 well tissue culture plates in numbers determined optimal for confluent monolayer growth (5,000 cells/well for HOS, HTB-186 Daoy; 10,000 cells/well for TC-71, RD, SK-N-AS, SK-N-DZ, LD; 30,000 cells/well for KCNR), with an automated, multichannel pipette system. Cells are incubated for 24 hours at 37 °C/5% CO2 then exposed to vehicle control (1.25% DMSO/H2O), VCR (0.1–1000 nM), ABT-751 (0.1 nM–100 μM), and in 4 cell lines (SK-N-AS, KCNR, RD, TC-71) combretastatin (0.1–1000 nM) for 72 hours. Cells are fixed with trichloroacetic acid (final concentration 10%) at 4 °C, washed, then dried at room temperature, stained with SRB in 1% acetic acid and dye is then solubilized with Tris base. Optical density measurements are performed at 540 and 405 nm dual wavelengths in a Bio-Tek EL 340 UV plate reader.
In Vivo
In vivo In this Calu-6 xenograft model, ABT-751 as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, ABT-751 shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, ABT-751 also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay In combination with 5-FU. [2] In dogs with lymphoma, ABT-751 exhibits the dose-limiting toxicities that included vomiting, diarrhea, anorexia, or some combination of these with a maximum tolerated dose (MTD) of 350 mg/m2 PO q24h. Furthermore, the mean AUC and Cmax for ABT-751 at the MTD of 350 mg/m2 is 5.55 μg-hour/mL and 0.9 μg/mL, respectively. [3]
Animal Research Animal Models Calu-6 NSCLC, HT-29 colon, and HCT-116 cells are injected into athymic mice.
Dosages 75 or 100 mg/kg/day
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00436852 Completed Disseminated Neuroblastoma|Recurrent Neuroblastoma Children''s Oncology Group|National Cancer Institute (NCI) January 2007 Phase 2
NCT00735878 Terminated Non Small Cell Lung Cancer|Lung Cancer Konstantin Dragnev|Abbott|Dartmouth-Hitchcock Medical Center September 2004 Phase 1|Phase 2

Chemical lnformation & Solubility

Molecular Weight 371.41 Formula

C18H17N3O4S
CAS No. 141430-65-1 SDF Download ABT-751 (E7010) SDF
Smiles COC1=CC=C(C=C1)S(=O)(=O)NC2=C(N=CC=C2)NC3=CC=C(C=C3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (199.24 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble


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