Size : 5 mg
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| GDC-0941 inhibits the activity of recombinant PI3K in vitro with IC50's of 0.003 µM (P110a), 0.033 µM (P110ß), 0.003 µM (P110d), 0.075 µM (P110γ), 0.58 µM (mTOR) and 1.23 µM (DNA-PK). GDC-0941 inhibited the growth of tumor cells in vitro with IC50's of 0.95 µM (U87MG), 0.07 µM (IGROV-1), 0.15 µM (DETROIT 562), 0.28 µM (PC3) and 0.54 µM (SKOV-3). GDC-0941 also inhibited the growth of U87 MG glioblastoma xenografts and IGROV-1 ovarian cancer xenografts in mice. Raynaud, F.I., 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. 8: 1725-1738 (2009). Soluble in DMSO at 66 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM buffers, serum, or other additives may increase or decrease the aqueous solubility GDC-0941 is a phosphatidylinositol 3-kinase (PI3K) inhibitor. Folkes, A.J., 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. 51: 5522-5532 (2008). |
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