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Description: ABI-274 is a novel, orally bioavailable, highly potent and selective tubulin/mitotic inhibitor (specifically a microtubule destabilizer) targeting the colchicine binding site, belonging to the so called colchicine binding site inhibitor (CBSI). It has shown potent anticancer activities in vitro and in vivo, as well as favorable pharkacokinetics such as good oral bioavailability.
References:
1. Chen J, Wang Z, Li CM, Lu Y, Vaddady PK, Meibohm B, Dalton JT, Miller DD, Li W. Discovery of novel 2-aryl-4-benzoyl-imidazoles targeting the colchicines binding site in tubulin as potential anticancer agents. J Med Chem . 2010 Oct 28; 53(20):7414-27. doi: 10.1021/jm100884b.
2. Wang J, Chen J, Miller DD, Li W. Synergistic combination of novel tubulin inhibitor ABI-274 and vemurafenib overcome vemurafenib acquired resistance in BRAFV600E melanoma. Mol Cancer Ther. 2014 Jan; 13(1):16-26. doi: 10.1158/1535-7163.MCT-13-0212.
3. Wang Z, Chen J, Wang J, Ahn S, Li CM, Lu Y, Loveless VS, Dalton JT, Miller DD, Li W. Novel tubulin polymerization inhibitors overcome multidrug resistance and reduce melanoma lung metastasis. Pharm Res. 2012 Nov; 29(11):3040-52. doi: 10.1007/s11095-012-0726-4. Epub 2012 Mar 13. PMID: 22410804
4. Li CM, Chen J, Lu Y, Narayanan R, Parke DN, Li W, Ahn S, Miller DD, Dalton JT. Pharmacokinetic optimization of 4-substituted methoxybenzoyl-aryl-thiazole and 2-aryl-4-benzoyl-imidazole for improving oral bioavailability. Drug Metab Dispos. 2011 Oct; 39(10):1833-9. doi: 10.1124/dmd.110.036616. Epub 2011 Jul 8. PMID: 21742898
Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.
All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.
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