产品
编 号:F358403
分子式:C17H12N2O
分子量:260.29
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
200
In-stock
5mg
440
In-stock
10mg
632
In-stock
50mg
2176
In-stock
100mg
3380
In-stock
结构图
联系客服
产品详情
生物活性:
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).

体内研究:
PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models.PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression.PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells.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.PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance.

体外研究:
PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro. PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity.PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis.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.PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells.
产品资料