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Biological Activity:
Potent, selective, orally bioavailable inhibitor of class I PI3 kinase (PI3K) under clinical trials, with IC50 values (nM) of 3, 33, 3, 75, 1230 and 580 for p110 α, β, δ and γ isoforms, DNA-PK and mTOR; water-soluble form.
References: online 1, 2, 3
AJ Folkes et al. 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. 2008, 51(18), 5522-32. [abstract]
FI Raynaud et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. Mol. Cancer Ther. 2009, 8(7), 1725-38. [abstract]
Chemical Name: 2-(1H-Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1ylmethyl)
-4-morpholin-4-yl-thieno[3,2-d]pyrimidine bismesylate
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