A potent inhibitor of mTOR
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GDC-0349

Item No. 24058

Technical Information
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
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:9): 0.1 mg/mlEthanol: 10 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).1 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.1,2 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 (Item No. 11600) or the MEK inhibitor cobimetinib (GDC-0973; Item No. 19563).

    WARNING This product is not for human or veterinary use.