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GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR, Ki = 3.8 nM). It is selective for mTOR over a panel of 266 kinases at a concentration of 1 µM. GDC-0349 inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in head and neck squamous cell carcinoma (HNSCC) cells via inhibition of mTOR complex 1 (mTORC1) and mTORC2 and induction of autophagy. Oral administration of GDC-0349 (10-80 mg/kg) inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner. It also reduces tumor growth in an A549 lung cancer mouse xenograft model when administered in combination with the PI3K inhibitor GDC-0941 (Cay-11600) or the MEK inhibitor cobimetinib (GDC-0973, Cay-19563).Formal Name: N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]-urea. CAS Number: 1207360-89-1. Molecular Formula: C24H32N6O3. Formula Weight: 452.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:9): 0.1 mg/ml, Ethanol: 10 mg/ml. lambdamax: 297 nm. SMILES: C[C@H]1COCCN1C2=NC(C3=CC=C(NC(NCC)=O)C=C3)=NC4=C2CCN(C5COC5)C4. InChi Code: InChI=1S/C24H32N6O3/c1-3-25-24(31)26-18-6-4-17(5-7-18)22-27-21-12-29(19-14-33-15-19)9-8-20(21)23(28-22)30-10-11-32-13-16(30)2/h4-7,16,19H,3,8-15H2,1-2H3,(H2,25,26,31)/t16-/m0/s1. InChi Key: RGJOJUGRHPQXGF-INIZCTEOSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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