VS-5584 Chemical Properties

Boiling point:

687.2±65.0 °C(Predicted)

Density 

1.48±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in H2O; ≥17.7 mg/mL in DMSO; ≥4.71 mg/mL in EtOH with ultrasonic

form 

solid

pka

4.53±0.10(Predicted)

color 

Light yellow to yellow

VS-5584 Usage And Synthesis

Description

Phosphatidylinositol 3-kinase (PI3K) signaling through Akt/PKB and the mammalian target of rapamycin (mTOR) controls gene expression related to cell proliferation, differentiation, and apoptosis. Increased activity of this pathway is important in many types of cancer. VS-5584 is a purine analog that inhibits mTOR (IC₅₀ = 37 nM) and PI3K (IC₅₀s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively) without relevant activity against more than 400 additional lipid and protein kinases. By inhibiting the phosphorylation of substrates downstream of PI3K and mTOR, VS-5584 demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.

target

mTOR

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