GI-149893
GI-149893 is a selective topoisomerase I (TopoI) inhibitor. GI-149893 prevents DNA religation and induces irreversible DNA damage in tumor cells. GI-149893 is promising for research of cancers (e.g., colon carcinoma HT-29/SW-48, breast MX-1, prostate PC-3 xenografts).
For research use only. We do not sell to patients.
- CAS No.: 149809-18-7
- Formula: C27H28N4O6
- Molecular Weight:504.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Topoisomerase Isoforms
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Biological Activity
Description
IC50 & Target
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Topoisomerase I |
Chemical Information
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CAS No. 149809-18-7
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Molecular Weight 504.53
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Formula C27H28N4O6
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SMILES
O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CN5CCN(C)CC5)C6=CC7=C(OCO7)C=C6N=C4C3=C2)=O
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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.
Protocols
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Purity & Documentation
References
[1]. Emerson DL, et al. In vivo antitumor activity of two new seven-substituted water-soluble camptothecin analogues. Cancer Res. 1995 Feb 1;55(3):603-9. [Content Brief]
[2]. Fan Y, et al. Molecular modeling studies of the DNA-topoisomerase I ternary cleavable complex with camptothecin. J Med Chem. 1998 Jun 18;41(13):2216-26. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)