ABT-751 hydrochloride
ABT-751 (E7010) hydrochloride 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 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 141450-48-8
- Formula: C18H18ClN3O4S
- Molecular Weight:407.87
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
1.111 μM
Compound: 47, ABT-751
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Anticancer activity against human A375 cells after 96 hrs by SRB assay
Anticancer activity against human A375 cells after 96 hrs by SRB assay
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[PMID: 21557538] |
| B16-F1 | IC50 |
2.127 μM
Compound: 47, ABT-751
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Anticancer activity against mouse B16-F1 cells after 96 hrs by SRB assay
Anticancer activity against mouse B16-F1 cells after 96 hrs by SRB assay
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[PMID: 21557538] |
| DU-145 | IC50 |
0.839 μM
Compound: 47, ABT-751
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Anticancer activity against human DU145 cells after 96 hrs by SRB assay
Anticancer activity against human DU145 cells after 96 hrs by SRB assay
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[PMID: 21557538] |
| LNCaP | IC50 |
0.658 μM
Compound: 47, ABT-751
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Anticancer activity against human LNCAP cells after 96 hrs by SRB assay
Anticancer activity against human LNCAP cells after 96 hrs by SRB assay
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[PMID: 21557538] |
| PC-3 | IC50 |
0.786 μM
Compound: 47, ABT-751
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Anticancer activity against human PC3 cells after 96 hrs by SRB assay
Anticancer activity against human PC3 cells after 96 hrs by SRB assay
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[PMID: 21557538] |
| PPC-1 | IC50 |
0.701 μM
Compound: 47, ABT-751
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Anticancer activity against human PPC1 cells after 96 hrs by SRB assay
Anticancer activity against human PPC1 cells after 96 hrs by SRB assay
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[PMID: 21557538] |
ABT-751 hydrochloride (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 hydrochloride (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 hydrochloride (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 hydrochloride [6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ABT-751 hydrochloride (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.
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Animal Model:xenograft models of neuroblastoma, osteosarcoma, Ewing sarcoma rhabdomyosarcoma, medulloblastoma and eight kidney cancer lines (six Wilms tumors, two rhabdoid)[7]
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Dosage:100 mg/kg
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Administration:Oral gavage (p.o.)
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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).
Chemical Information
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CAS No. 141450-48-8
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Molecular Weight 407.87
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Formula C18H18ClN3O4S
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SMILES
COC1=CC=C(C=C1)S(=O)(NC2=C(N=CC=C2)NC3=CC=C(C=C3)O)=O.[H]Cl
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Synonyms
E7010 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Huang SM et al.,Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling., Nature. 2009 Oct 1;461(7264):614-20. [Content Brief]
[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]. 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]
[7]. Morton CL, et al. Evaluation of ABT-751 against childhood cancer models in vivo. Invest New Drugs. 2007;25(4):285-295. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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