Companies
MedChemExpress LLC (MCE)
Products
MedChemExpress - Model PFK-015 - ...

MedChemExpress - Model PFK-015 - 4382-63-2

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].

PFK-015

MCE China：PFK-015

Brand：MedChemExpress (MCE)

Cat. No.HY-12204

CAS：4382-63-2

Purity：99.80%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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).

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].

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]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PFK-015 Related Antibodies

References：

[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. [Content Brief]

[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.

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。