GDC-0941
pan-PI3K inhibitor / GDC-0941 is a potent and selective inhibitor of class I phosphatidylinositol-3-kinases (PI3K) with significant antitumor activity – IC50’s: PI3Kα = 3nM, PI3Kβ = 33 nM, PI3Kδ = 3 nM, PI3Kγ = 75 nM.1,2 GDC-0941 is the chemical probe of choice for the pan-inhibition of class I PI3K’s.3 Currently in clinical trials.4
Biochemicals & reagents
957054-30-7
Pictilisib
1) Folkes et al. (2008), The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine(GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer; J.Med.Chem. 51 5522 2) Raynaud et al. (2009), Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinase: from PI-103 through PI-540, PI620 to the oral agent GDC-0941; Mol.Cancer Ther. 8 1725 3) Knapp et al. (2013), A public-private partnership to unlock the untargeted kinome; Nat.Chem.Biol. 9 3 4) Sarker et al. (2015), First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors; Clin.Cancer Res. 21 77
-20°C
TARGET: Kinase -- PATHWAY: PI3K -- RESEARCH AREA: Cancer stem cells -- DISEASE AREA: Cancer