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GDC-0084 1382979-44-3

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Synonyms ：
Appearance ：
Chemical Formula ：
C18H22N8O2
Solubility ：
Molecular Weight ：
382.42
Storage and Stability ：
in stock
CAS No. ：
1382979-44-3
Purity ：
98%+
Introduction
GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

GDC-0084 has excellent human metabolic stability in microsomal and hepatocyte incubations and demonstrated inhibition of pAKT, a key signal within the PI3K pathway, in normal brain tissue. GDC-0084 is shown to inhibit the proliferation of several glioma cells in vitro with IC50 ranging from 0.3 to 1.1 μM. GDC-0084 binding to plasma proteins is low, with a free fraction (%) of 29.5±2.7 (n=3) in CD-1 mouse plasma, when tested at 5 μM. Binding to brain tissues from CD-1 mice is higher, with a free fraction of 6.7% (±1; n=3).

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