VS-5584 (SB2343) (Synonyms: SB-2343;VS5584;VS 5584;SB2343;SB 2343) |
| Catalog No.GC17771 |
A selective PI3K/mTOR kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1246560-33-7
Sample solution is provided at 25 µL, 10mM.
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VS-5584 (SB2343), a purine analog, is a novel small-molecule inhibitor of both mammalian target of rapamycin (mTOR) kinase and all class I phosphoinostide 3-kinase (PI3K) isoforms that ATP-competitively inhibits the activity of mTOR, PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ with values of 50% inhibition concentration IC50 of 37 nmol/L, 16 nmol/L, 68 nmol/L, 25 nmol/L and 42 nmol/L respectively. VS-5585 robustly modulates the cellular PI3K/mTOR pathway, one of the most commonly activated signaling pathways in human cancer, through inhibition of phosphorylation of substrates downstream of PI3K and mTORC1/2. Moreover, VS-5584 has been found to dose-dependently inhibit PI3K/mTOR signaling in tumor tissue resulting in tumor growth inhibition in human xengograft models.
Reference
Hart S, Novotny-Diermayr V, Goh KC, Williams M, Tan YC, Ong LC, Cheong A, Ng BK, Amalini C, Madan B, Nagaraj H, Jayaraman R, Pasha KM, Ethirajulu K, Chng WJ, Mustafa N, Goh BC, Benes C, McDermott U, Garnett M, Dymock B, Wood JM. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61. doi: 10.1158/1535-7163.MCT-12-0466. Epub 2012 Dec 27.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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