PFK-015

PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC₅₀ value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC₅₀ value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC)^[1][2]. IC50 & Target: IC50: 110 nM (recombinant PFKFB3); IC50: 20 nM (PFKFB3 activity in cancer cells)^[2] In Vitro: PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro^[1].
PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity^[1].
PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis^[1].
PFK-015 potently inhibits recombinant PFKFB3 with an IC₅₀ value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC₅₀ value of 20 nM^[2].
PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells^[2]. In Vivo: PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models^[1].
PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression^[1].
PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 ⁺ T cells^[1].
PFK-015 enhances the efficacy of ESCC by enhancing CD8 ⁺ T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG^[1].
PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance^[2].