|
Biological Activity:
Selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms and apparent Ki of 17.3 nM for human mTOR. GDC-0980 has excellent pharmacokinetic and pharmaceutical properties and demonstrates broad activity in xenograft cancer models (breast, ovarian, lung, and prostate).
References: online
JJ Wallin et al. GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway. Mol. Cancer Ther. 2011, 10(12), 2426-2436. [online]
AJ Wagner et al. A first-in-human phase I study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QD in patients with advanced solid tumors. J. Clin. Oncol. 2011, 29 (suppl; abstr 3020). [online]
DP Sutherlin et al. Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer. J. Med. Chem. 2011, 54(21), 7579-87. [online]
Chemical Name: (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one
|
