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STEMCELL Technologies GDC-0941, Size: 10 mg

Supplier: STEMCELL Technologies 73152

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.).CANCER RESEARCH· 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.).
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