PF-4989216 (C09-1017-186)

InformationPF-4989216 is a potent and selectivePI3Kinhibitor withIC50of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.Targetsp110δ (Cell-free assay); p110α (Cell-free assay); p110γ (Cell-free assay) 1 nM; 2 nM; 65 nMIn vitroPF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis.In vivoIn SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity.Cell Research(from reference)Cell lines：NCI-H69, NCI-H1048, NCI-H1436, NCI-H82, NCI-H254, NCI-H526, NCI-H1963, NCI-H146, NCI-H841, Lu99A, Lu134B, and Lu134A cells. Concentrations：~10 μM Incubation Time：72 hours. Specifications and Purity: 99%. Molecular Formula: C18H13FN6OS. Molecular Weight: 380.4. PubChem CID: 51033720. Isomeric SMILES: C1COCCN1C2=C(C(=C(S2)C3=NC=NN3)C4=C(C=C(C=C4)C#N)F)C#N. Related Document: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/P413810-SCI_a2ab362fa78a170480bfddd50076a4a4.pdf.