371935-74-9

Solubility:Soluble in DMSO

Storage:-20C 2 years

Biologieal

A selective class I PI3K inhibitor; it inhibits PI3K p110 isoforms, mTOC1 and also DNA-PK; a valuable tool compound.Inhibitor of DNA-PK, PI 3-kinase (p110α) and mTOR (IC₅₀ values are 2, 8, 20, 26, 48, 83, 88, 150, 850, 920, ~ 1000 and 2300 nM for DNA-PK, p110α, mTORC1, PI3KC2β, p110δ, mTORC2, p110β, p110γ, ATR, ATM, PI3KC2α and hsVPS34 respectively). Inhibits growth of human tumor xenografts in mice in vivo.

Reference

Fan et al (2006) A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell 9 341. Knight et al (2006) A pharmacological map of the PI3-K family defines a role for p110a in insulin signaling. Cell 125 733. Raynaud et al (2007) Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositol 3-kinase. Cancer Res. 67 5840.