包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Cell lines | human Ovarian Cancer cell lines (HeyA8 and HeyA8MDR), Cervical cancer cell line (OV2008, C13) |
Preparation Method | Cells were treated with PFK158, carboplatin (CBPt), Paclitaxel (PTX) alone and in combination, and Phosphatidyl‐serine externalization was analyzed by double staining the cells with FITC‐Annexin V and PI. |
Reaction Conditions | 10 μM PFK-158 for 24h. |
Applications | PFK-158 treatment sensitizes chemoresistant cells (C13) and induces cell death. The combined treatment of PFK158 and CBPt resulted in significant increase in apoptosis in C13 (45%) compared to OV2008 cells (24.6%). Similar analysis using a combination of PFK158 and PTX showed a marked increase in apoptosis in the HeyA8MDR (70%) cells compared to HeyA8 (48%), respectively. |
Animal models | Endometrial cancer (EC) mouse xenograft models |
Preparation Method | HEC-1B and ARK-2 cells were subcutaneously injected. Following the detection of palpable tumors, the mice were treated with vehicle, PFK158 alone 2×/week, carboplatin (CBPt) alone 1×/week, or both for 14 days. |
Dosage form | 35mg/kg PFK-158, intraperitoneal(i.p.) injection |
Applications | A significant reduction of tumor growth, tumor volume and tumor weight was observed at day 28 in both PFK158 alone and combination groups. H&E staining results demonstrated that PFK158- and combination treatment significantly increased tumor necrosis compared to control |
产品描述 | PFK-158 is a potent and selective PFKFB3 inhibitor, which shows extensive anti-tumor activity by reducing the uptake of glucose in cancer cells, the production of ATP, the release of lactic acid and inducing apoptosis and autophagy[1]. PFK-158 suppressed cell viability in a dose- and time-dependent manner in EC cells. Co-treatment with PFK158 (5 μM) and CBPt led to a significant increase in the percentage of apoptotic cells in HEC-1B and ARK-2. Furthermore, Western blot analysis revealed that the active form of PARP was significantly increased upon co-treatment, compared to single treatment alone, further demonstrating that the combination treatment enhances cell apoptosis[2] The efficacy of PFK158 alone and in combination with carboplatin (CBPt) was evaluated on primary tumor growth and metastasis in HeyA8MDR‐earing nude mice i.p. A marked reduction of tumor growth was observed in the combination treatment.PFK-158 with CBPt significantly reduced ascites and reduced LDs in tumor tissue as seen by immunofluorescence and transmission electron microscopy compared to untreated mice[3] References: |