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Apitolisib (GDC-0980)

Product Specifications

CAS Number

1032754-93-0

Synonyms

RG7422, GNE 390

Target

MTOR

Applications

PI3K/Akt/mTOR

Smiles

CC1=C (SC2=C1N=C (N=C2N3CCOCC3) C4=CN=C (N=C4) N) CN5CCN (CC5) C (=O) C (C) O

Molecular Formula

C23H30N8O3S

Additionnal 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.

Storage Conditions

2 years -80 in solvent

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