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PFK-158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3), which plays a crucial role in regulating glycolysis. It has demonstrated the ability to inhibit PFKFB3 and glycolysis in various cell lines, as well as suppress the growth of leukemia cells in vitro. Additionally, PFK-158 has shown potential in reducing tumor volume in different cancer models and enhancing the activity of certain antibodies in the treatment of melanoma.

1462249-75-7

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1462249-75-7 Usage

Uses

Used in Cancer Treatment:
PFK-158 is used as an inhibitor for PFKFB3 in cancer treatment, specifically targeting leukemia cells. It has shown to effectively inhibit the growth of leukemia cells in vitro (IC50 = 0.33 μM for Jurkat cells) and reduce tumor volume in CT-26 murine colon carcinoma syngeneic model and a BxPC-3 pancreatic cancer mouse xenograft model.
Used in Enhancing Antibody Activity:
PFK-158 is used as an enhancer for the anti-CTLA-4 antibody in the B16/F10 mouse model of melanoma. By inhibiting PFKFB3, PFK-158 can potentially improve the efficacy of the anti-CTLA-4 antibody, providing a more effective treatment option for melanoma patients.
Used in Research and Development:
PFK-158 is used as a research tool for studying the role of PFKFB3 in glycolysis and its potential as a therapeutic target in various types of cancer. Its ability to inhibit PFKFB3 and glycolysis in Jurkat cells (IC50s = 1.6 and 0.847 μM, respectively) makes it a valuable compound for investigating the underlying mechanisms of cancer cell metabolism and the development of novel cancer therapies.

Check Digit Verification of cas no

The CAS Registry Mumber 1462249-75-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,6,2,2,4 and 9 respectively; the second part has 2 digits, 7 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1462249-75:
(9*1)+(8*4)+(7*6)+(6*2)+(5*2)+(4*4)+(3*9)+(2*7)+(1*5)=167
167 % 10 = 7
So 1462249-75-7 is a valid CAS Registry Number.

1462249-75-7Downstream Products

1462249-75-7Relevant academic research and scientific papers

PFKFB3 INHIBITOR AND METHODS OF USE AS AN ANTI-CANCER THERAPEUTIC

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, (2013/10/21)

A novel compound, (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one, is provided herein. (E)-1-(pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)-prop-2-en-1-one is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-biphosphata

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