GDC0980, a orally-available, thienopyrimidine-based, ATP-competitive dual inhibitor of PI3K class I isoforms (IC50 of 5, 27, 7, and 14 nM for PI3Ka, b, d, and g) and mTOR (Ki of 17 nM). [1] GDC0980 potently inhibits signal transduction (Thr308, Ser473) downstream of both PI3K and mTOR and showed most potent antitumor activity in breast, prostate, and lung cancer (IC50
Technical information:
| Chemical Formula: | C23H30N8O3S | |
| CAS #: | 1032754-93-0 | |
| Molecular Weight: | 498.6 | |
| Purity:> 98% | ||
| Appearance: | White | |
| 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 | |
| Solubility: | Up to 40 mM in DMSO | |
| Synonyms: | GDC-0980, GDC0980, RG7422, |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | 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, 7579-7587. Pubmed ID:21981714 |
| 2. | 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, 2426-2436. Pubmed ID:21998291 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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