| Identification | Back Directory | [Name]
E-7010 monohydrochloride | [CAS]
141450-48-8 | [Synonyms]
ABT-751 hydrochloride
E-7010 monohydrochloride
ABT-751 monohydrochloride
ABT-751 hydrochloride >=98% (HPLC)
N-[2-[(4-Hydroxyphenyl)aMino]-3-pyridyl]-4-MethoxybenzenesulfonaMide hydrochloride
N-{2-[(4-hydroxyphenyl)aMino]pyridin-3-yl}-4-MethoxybenzenesulfonaMide hydrochloride
N-[2-[(4-Hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide monohydrochloride
BenzenesulfonaMide, N-[2-[(4-hydroxyphenyl)aMino]-3-pyridinyl]-4-Methoxy-, Monohydrochloride | [Molecular Formula]
C18H18ClN3O4S | [MDL Number]
MFCD19440802 | [MOL File]
141450-48-8.mol | [Molecular Weight]
407.871 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥15mg/mL | [form ]
powder | [color ]
pink to purple | [InChI]
1S/C18H17N3O4S.ClH/c1-25-15-8-10-16(11-9-15)26(23,24)21-17-3-2-12-19-18(17)20-13-4-6-14(22)7-5-13;/h2-12,21-22H,1H3,(H,19,20);1H | [InChIKey]
KWQWWUXRGIIBAS-UHFFFAOYSA-N | [SMILES]
Cl.COc1ccc(cc1)S(=O)(=O)Nc2cccnc2Nc3ccc(O)cc3 |
| Safety Data | Back Directory | [Hazard Codes ]
Xn | [Risk Statements ]
22-36/37/38 | [Safety Statements ]
26 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Acute Tox. 4 Oral
Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| Hazard Information | Back Directory | [Uses]
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[1][2][3][4][5][6][7][8][9]. | [Biological Activity]
ABT-751 is an orally bioavailable vascular disrupting agent (VDA) with a broad spectrum of antitumor activity. It binds to the colchicine binding site on β-tubulin and inhibits polymerization of microtubules.''ABT-751a sulfonamide antimitotic agentis under clinical trials to tre at patients with various malignancies including refractory hematologic malignanciesnon-small cell lung cancer (NSCLC)and colon cancer. | [in vivo]
ABT-751 hydrochloride (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 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].
| 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).
|
| [References]
[1] Huang SM et al.,Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling., Nature. 2009 Oct 1;461(7264):614-20. DOI:10.1038/nature08356
[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. DOI:10.4161/cbt.19594
[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. DOI:10.1111/j.1939-1676.2012.00892.x
[5] Gaynon PS, Harned TM; for the Therapeutic Advances in Childhood LeukemiaLymphoma (TACL) Consortium. DOI:10.1097/MPH.0b013e3182532446
[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. PMID:9242451
[7] Morton CL, et al. Evaluation of ABT-751 against childhood cancer models in vivo. Invest New Drugs. 2007;25(4):285-295. DOI:10.1007/s10637-007-9042-y
[8] 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. |
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| Company Name: |
NCE Biomedical Co.,Ltd.
|
| Tel: |
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15748/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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