Catalog No.: PC-38635Not For Human Use, Lab Use Only.
NVP-CLR457 (CLR457) is a potent, orally bioavailable, non-CNS-penetrant pan-class I PI3K inhibitor with IC50 values of 89 nM, 56 nM, 39 nM and 230 nM for p110α, p110β, p110δ and p110γ isoforms, respectively.
NVP-CLR457 (CLR457) is a potent, orally bioavailable, non-CNS-penetrant pan-class I PI3K inhibitor with IC50 values of 89 nM, 56 nM, 39 nM and 230 nM for p110α, p110β, p110δ and p110γ isoforms, respectively.
NVP-CLR457 (CLR457) also inhibited the most common forms of PIK3CA mutant isoforms: E545K (helical domain mutation) and H1047R (kinase domain mutation).
NVP-CLR457 (CLR457) demonstrated antitumor activity in multiple tumor xenograft models with constitutively active PI3K pathway.
