Name:Apitolisib (GDC-0980)
Synonyms:RG7422, GNE 390
CAS Number:1032754-93-0
Formula:C23H30N8O3S
M.w.:498.6
DMSO (mg/mL)Max Solubility:20
DMSO (mM)Max Solubility:40.11
Form:free base
SMILES:CC(O)C(=O)N1CCN(CC1)CC2=C(C)C3=NC(=NC(=C3S2)N4CCOCC4)C5=CN=C(N)N=C5
ALogP:1.013
Target:Apoptosis related,Autophagy,mTOR,PI3K
Pathway:PI3K/Akt/mTOR
Information:Apitolisib (GDC-0980, RG7422, GNE 390) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. Also a mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib activates autophagy and apoptosis simultaneously in pancreatic cancer cells. Phase 2.
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