| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 110 nM (recombinant PFKFB3); IC50: 20 nM (PFKFB3 activity in cancer cells) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | PFK-015 | ||||||||||||
| CAS | 4382-63-2 | ||||||||||||
| Formula | C17H12N2O | ||||||||||||
| Molar Mass | 260.29 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Jia Bo Zheng, et al. Glucose metabolism inhibitor PFK-015 combined with immune checkpoint inhibitor is an effective treatment regimen in cancer. Oncoimmunology. 2022 May 25;11(1):2079182. [2]. Brian Clem, et al. Characterization of a novel small molecule antagonist of 6-phosphofructo-2-kinase that suppresses glucose metabolism and tumor growth. ORAL PRESENTATIONS - PROFFERED ABSTRACTS| APRIL 15 2011. |