A potent inhibitor of mTOR (Ki = 3.8 nM); selective for mTOR over a panel of 266 kinases at a concentration of 1 μM; inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in HNSCC cells; oral administration inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner (10-80 mg/kg)

GDC-0349 – 500 µg

Brand:
Cayman
CAS:
1207360-89-1
Storage:
-20
UN-No:
De Minimis - 3077 / 9

GDC-0349 is a potent inhibitor of the mammalian target of rapamycin (mTOR; Ki = 3.8 nM).{41444} 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.{41444,41445} 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).  

 

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SKU: 24058 - 500 µg Category:

Description

A potent inhibitor of mTOR (Ki = 3.8 nM); selective for mTOR over a panel of 266 kinases at a concentration of 1 μM; inhibits proliferation of PC3 prostate cancer cells in vitro (EC50 = 270 nM) and induces caspase-dependent apoptosis in HNSCC cells; oral administration inhibits tumor growth in MCF7-neo/Her-2 breast and PC3 prostate cancer mouse xenograft models in a dose-dependent manner (10-80 mg/kg)

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

Synonyms: 

Molecular weight: 452.6

CAS: 1207360-89-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Endomembrane System & Vesicular Trafficking|Autophagy

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