PFK-015

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PFK-015 是 PFKFB3 的有效抑制剂 (IC50: 110 nM)，并抑制 Y 细胞中的 PFKFB3 活性 (IC50: 20 nM)。

PFK-015 is a potent inhibitor of PFKFB3. The preliminary results in a U87GM xenograft model have shown that PFK-015 has comparable activity to Temozolomide. PFK-015 inhibits glucoseuptake by tumors.

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.

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.

PFK015 | PFK 015 | PFK015.

Others

Other Targets

PFKFB3

Cancer

——

4382-63-2

260.29

C17H12N2O

>98% (HPLC)

DMSO : 25.2 mg/mL 96.82 mM; H2O : < 0.1 mg/mL

C(=O)(/C=C/c1nc2c(cc1)cccc2)c1ccncc1

(E)-3-(pyridin-3-yl)-1-(quinolin-3-yl)prop-2-en-1-one

(-20℃)

With Ice Pack

≥ 2 years