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Cat. No. Name Size Price Add Cart
KI0865VS-55845 mg$831.6

Chemical Characteristic

Product NameVS-5584
SynonymsSB2343
CAS No.1246560-33-7
Molecular Weight 354.41
FormulaC17H22N8O
Chemical Structure

Biological activities

VS-5584 is a selective dual PI3K/mTOR inhibitor that potently inhibits mTOR kinase PI3K isoforms. VS-5584 inhibits mTOR, PI3Ka, PI3Ka mtH1047, PI3Kβ, PI3Kδ and PI3Kγ with IC50 of 3.4, 2.6, 3.3, 21, 2.7 and 3.0 nM, respectively. VS-5584 preferentially inhibits cancer stem cells with an EC50 of 15 nM in HMLE breast cancer cells. Accordingly, VS-5584 preferentially decreases CD44Hi/CD24Lo cells in an HMLER immortalized mammary cancer cell line. In SUM159 cells, VS-5584 effectively eliminates the cancer stem cell side population.[1] In the FLT3-ITD harboring MV4-11 cells, VS-5584 blocks pAkt (S473) and pAkt (T308) with IC50 of 12 and 13 nM, respectively. The IC50 of VS-5584 for pS6 (S240/244), pAkt (S473), and pAkt (T308) are 20, 23, and 15 nM, respectively. [2] In mice bearing triple negative breast cancer tumors, oral dosing of VS-5584 decreases tumor cancer stem cells and induces tumor regression in taxane-resistant models. [1]In a PTENnull human prostate PC3 xenograft model, treatment with VS-5584 leads to significant tumor growth inhibition (TGI) of 79% and 113% for 11 and 25 mg/kg, respectively. In a FLT3-ITD AML xenograft model, VS-5584 treatment induces dose-dependent inhibition of tumor growth (28% for 3.7 mg/kg and 76% for 11 mg/kg). [2]

Protocols

For in vivo studies, VS-5584 is prepared in 0.5% methylcellulose (w/v) and 0.1% Tween-80 in H2O (MC/Tween). [2]

References

[1] Pachter JA, et al. The pan-PI3K/mTOR kinase inhibitor VS-5584 preferentially targets cancer stem cells in breast cancer models. 2012. 閵嗏偓閵嗏偓
[2] Hart S, et al. VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013, 12(2): 151-161. 閵嗏偓閵嗏偓

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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