Home Cytoskeletal Signaling Microtubule Associated inhibitor ABT-751 (E7010)

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ABT-751 (E7010) Microtubule Associated inhibitor

Cat.No.S1165

ABT-751 (E7010) binds to the colchicine site on β-tubulin and inhibits polymerization of microtubules. It is 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) Microtubule Associated inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 371.41

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Quality Control

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

Cell Culture, Treatment & Working Concentration

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
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
NCI-H460 cell Proliferation assay Antiproliferative activity against human lung carcinoma NCI-H460 cell line (MDR(+)), IC50=0.35 μM
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
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
human HL60 cells Proliferation assay Antiproliferative activity against human HL60 cells, IC50=0.34 μM
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
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
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
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
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
HT-29 cells Proliferation assay 72 h Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.21 μM
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
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
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
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
human A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50=1.31 μM
ACHN cells Cytotoxicity assay 48 h Cytotoxicity against human ACHN cells after 48 hrs by MTT assay, IC50=2.13 μM
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50=1.25 μM
HT-29 cells Cytotoxicity assay 48 h Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay, IC50=1.62 μM
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
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
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
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
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
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
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
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
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
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
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
DU145 cells Cytotoxicity assay 48 h Cytotoxicity against human DU145 cells after 48 hrs by MTT assay， GI50=1.81 μM
human SKBR3 cells Growth inhibition assay 48 h Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay, IC50=0.74 μM
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Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 12 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 371.41 Formula

C18H17N3O4S

 Storage (From the date of receipt)
CAS No. 141430-65-1 Download SDF Storage of Stock Solutions

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

Mechanism of Action

Features
An orally bioavailable tubulin-binding and antimitotic sulfonamide.
Targets/IC50/Ki
Microtubules
In vitro
In vitro, ABT-751 (E7010) shows selective cytotoxicity with IC50 values of 0.6–2.6 μM in neuroblastoma and 0.7–4.6 μM in other solid tumor cell lines. Furthermore, it 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 its IC90 concentration.
In vivo
In this Calu-6 xenograft model, ABT-751 (E7010) as a single agent at 100 and 75 mg/kg/day shows significant antitumor activity, while in combination with cisplatin, it shows a dose-dependent enhancement in growth delay. In the HT-29 colon xenograft model, this compound also shows significant antitumor activity as a single agent and produced a dose-dependent enhancement in growth delay in combination with 5-FU. In dogs with lymphoma, it 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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