Topovale

TargetMol
Product Code: TAR-T9088
Supplier: TargetMol
CodeSizePrice
TAR-T9088-1mg1mg£141.00
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TAR-T9088-5mg5mg£214.00
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TAR-T9088-10mg10mg£275.00
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TAR-T9088-25mg25mg£440.00
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TAR-T9088-50mg50mg£613.00
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TAR-T9088-100mg100mg£843.00
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Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

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Further Information

Bioactivity:
Topovale is a potent inhibitor of topoisomerase I. Topovale inhibits hypoxia-mediated accumulation of hypoxia-inducible factor-1alpha. Topovale exhibited low nM cytotoxicity against a panel of cancer cells. Topovale cytotoxicity as well as Topovale-induced apoptosis was reduced > 100-fold in CPT-resistant topoisomerase I (TOP1)-deficient P388/CPT45 cells as compared with P388 cells.
CAS:
500214-53-9
Formula:
C23H23N3O5
Molecular Weight:
421.453
Pathway:
DNA Damage/DNA Repair
Purity:
0.9994
SMILES:
COc1cc2c3cnc4cc5OCOc5cc4c3n(CCN(C)C)c(=O)c2cc1OC
Target:
Topoisomerase

References

Feng W, Satyanarayana M, Tsai YC, Liu AA, Liu LF, LaVoie EJ. Novel topoisomerase I-targeting antitumor agents synthesized from the N,N,N-trimethylammonium derivative of ARC-111, 5H-2,3-dimethoxy-8,9-methylenedioxy-5-[(2-N,N,N-trimethylammonium)ethyl]dibenzo[c ,h][1,6]naphthyridin-6-one iodide. Eur J Med Chem. 2009 Sep;44(9):3433-8. doi: 10.1016/j.ejmech.2009.02.004. PubMed PMID: 19299037; PubMed Central PMCID: PMC2766012. Kurtzberg LS, Battle T, Rouleau C, Bagley RG, Agata N, Yao M, Schmid S, Roth S, Crawford J, Krumbholz R, Ewesuedo R, Yu XJ, Wang F, Lavoie EJ, Teicher BA. Bone marrow and tumor cell colony-forming units and human tumor xenograft efficacy of noncamptothecin and camptothecin topoisomerase I inhibitors. Mol Cancer Ther. 2008 Oct;7(10):3212-22. doi: 10.1158/1535-7163.MCT-08-0568. PubMed PMID: 18852125. Li TK, Houghton PJ, Desai SD, Daroui P, Liu AA, Hars ES, Ruchelman AL, LaVoie EJ, Liu LF. Characterization of ARC-111 as a novel topoisomerase I-targeting anticancer drug. Cancer Res. 2003 Dec 1;63(23):8400-7. PubMed PMID: 14679002. Zhou W, Dai Z, Chen Y, Wang H, Yuan Z. High-Dimensional descriptor selection and computational QSAR modeling for antitumor activity of ARC-111 analogues Based on Support Vector Regression (SVR). Int J Mol Sci. 2012;13(1):1161-72. doi: 10.3390/ijms13011161. PubMed PMID: 22312310; PubMed Central PMCID: PMC3269744.