PI3K/AKT pathway inhibitor; Inhibits Class I PI3Ks
CAS
957054-30-7
Synonyme
GNE 0941; Pictilisib; Pictrelisib
Quantité
10 mg
Formule moléculaire
C23H27N7O3S2
Pureté
≥98%
Marque
STEMCELL Technologies
Caractéristiques principales
GDC-0941 is an inhibitor of phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K)
It inhibits class I catalytic subunits of PI3K p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively, by binding near the ATP binding pocket (Folkes et al.; Berndt et al.) It shows selectivity against class II, III, and IV PI3K isoforms as well, but with lower efficacy; for example, it inhibits phosphatidylinositol-4-phosphate 3-kinase C2 domain subunit β (C2β, Class II) and mammalian target of rapamycin (mTOR, Class IV) in the high nanomolar range and most others in the micromolar range (Folkes et al.)
Inhibits proliferation of multiple cancer cell lines, such as U87MG (glioblastoma), PC3 (prostate) and MDA-MB-361 (breast) lines, in vitro and in mouse xenograft models (Folkes et al.; Raynaud et al.; O'Brien et al.)
Induces apoptosis and inhibits xenograft tumor growth in combination with a MAP/ERK kinase (MEK) inhibitor GDC-0973 (Hoeflich et al.)
