Formulation: A solid
Formal Name: (3R)-1′-[3-(3,4-dihydro-1,5-naphthyridin-1(2H)-yl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-spiro[benzofuran-2(3H),4′-piperidin]-3-amine
Purity: ≥98%
Formula Markup: C25H26N8O
Formula Weight: 454,5
Shelf life (days): 1460
CAS Number: 2377352-49-1
Notes: GDC-1971 is an inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = E76K; IC50 = 0.17 µM). GDC-1971 reduces the levels of phosphorylated ERK in a reporter assay using KYSE-520 esophageal cancer cells (IC90 = 0.012 µM) and inhibits proliferation of the same cells (IC50 = 0.32 µM). In vivo, GDC-1971 (30 or 100 mg/kg two times per day) reduces tumor volume in KYSE-520 and NCI H358 non-small cell lung cancer (NSCLC) mouse xenograft models.