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VS-5584 (SB2343)MTOR/P13K inhibitor,potent and selective

VS-5584 (SB2343)

Catalog No. A3927
Size Price Stock Qty
10mM (in 1mL DMSO) $99.00 In stock
Evaluation Sample $28.00 In stock
5mg $90.00 In stock
10mg $120.00 In stock
50mg $400.00 In stock
5mg $500.00 Out of stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

VS-5584

Biological Activity

Description VS-5584 (SB2343) is a potent and selective dual inhibitor of PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.
Targets mTOR PI3Kα PI3Kα-H1047 PI3Kβ PI3Kδ PI3Kγ
IC50 3.4 nM 2.6 nM 3.3 nM 21 nM 2.7 nM 3.0 nM

VS-5584 (SB2343) Dilution Calculator

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Chemical Properties

Cas No. 1246560-33-7 SDF Download SDF
Synonyms SB-2343;VS5584;VS 5584;SB2343;SB 2343
Chemical Name 5-(8-methyl-2-morpholin-4-yl-9-propan-2-ylpurin-6-yl)pyrimidin-2-amine
Canonical SMILES CC1=NC2=C(N=C(N=C2N1C(C)C)N3CCOCC3)C4=CN=C(N=C4)N
Formula C17H22N8O M.Wt 354.41
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

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.