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PFK-015

CAS No.4382-63-2
Chemical Name:PFK-015
CBNumber:CB72705092
Molecular Formula:C17H12N2O
Formula Weight:260.29
MOL File:4382-63-2.mol

PFK-015 Property

Boiling point 464.4±45.0 °C(Predicted)
Density 1.237±0.06 g/cm3(Predicted)
storage temp. Sealed in dry,2-8°C
solubility DMSO: soluble10mg/mL, clear
pka 3.11±0.61(Predicted)
form powder
color white to beige
Stability Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
UNSPSC Code 12352200
NACRES NA.77

Safety

Hazard Codes :Xi
Risk Statements :36/37/38
Safety Statements :26-36/37/39
WGK Germany :3

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H315-H319-H335
Precautionary statements P261-P305+P351+P338

PFK-015 Price More Price(2)

Brand: Sigma-Aldrich(India)
Product number: SML1009
Product name : PFK15
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: ₹11528.63
Updated: 2022/06/14
Buy: Buy

Brand: Sigma-Aldrich(India)
Product number: SML1009
Product name : PFK15
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: ₹46515.03
Updated: 2022/06/14
Buy: Buy

PFK-015 Chemical Properties,Usage,Production

Description PFK15 (4382-63-2) is an inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3).? PFKFB3 is constitutively expressed by neoplastic cells and is required for the high glycolytic rate (Warburg Effect) of these cells. PFK15 inhibits PFKFB3 (IC50?= 207 nM) without inhibiting 96 other kinases.1?PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growth?in vitro?and?in vivo.?PFK15 has been shown to inhibit tumor growth in various cancer models.2,3
Uses PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells.
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].
storage Store at -20°C
References 1) Clem?et al.?(2013),?Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol. Cancer Ther.?12?1461 2) Zhu?et al. (2016),?PFK15,a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer; PLoS One?11?e0163768 3) Li?et al. (2017),?Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma; J. Exp. Clin. Cancer Res.?36?7