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GDC-0941 is a pan-PI3K inhibitor. When combined with paclitaxel, GDC-0941 exhibits antitumor activity in patients with locally recurrent or metastatic breast cancer. It also increases apoptosis in several cell lines of uveal melanoma in combination with the mTOR inhibitor everolimus.
| Cas No. | 957054-30-7 |
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| Purity | ≥98% |
| Formula | C23H27N7O3S2 |
| Formula Wt. | 513.64 |
| IUPAC Name | 2-(1H-Indazol-4-yl)-6-{[4-(methylsulfonyl)-1-piperazinyl]methyl}-4-(4-morpholinyl)thieno[3,2-d]pyrimidine |
| Synonym | GNE-0941, Pictilisib, Pictrelisib, RG7321 |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Folkes A., Ahmadi K., 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(18):5522-32 (2008). PMID: 18754654.
Schoffski P., Cresta S., et al. A phase Ib study of pictilisib (GDC-0941) in combination with paclitaxel, with and without bevacizumab or trastuzumab, and with letrozole in advanced breast cancer. Breast Cancer Res. 20(1):109 (2018). PMID: 30185228.
Amirouchene-Angelozzi N., Frisch-Dit-Leitz E., et al. The mTOR inhibitor Everolimus synergizes with the PI3K inhibitor GDC0941 to enhance anti-tumor efficacy in uveal melanoma. Oncotarget. 7(17):23633-46 (2016). PMID: 26988753.