PFK-015|PFK15,PFK 15|PFKFB3 inhibitor

Cas No.:	4382-63-2
Chemical Name:	(E)-3-(pyridin-3-yl)-1-(quinolin-3-yl)prop-2-en-1-one
Synonyms:	PFK015,PFK15,PFK 15,PFK-15
SMILES:	C1=CN=CC=C1C(=O)/C=C/C1=CC=C2C=CC=CC2=N1
Formula:	C₁₇H₁₂N₂O
M.Wt:	260.29
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM.PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents, and suppresses tumor glucose metabolism and growth in an aggressive mouse model of non-small cell lung cancer. PFK-015 is not a Pgp substrate as determined by transport and cell permeability assays in Caco-2 and MDCK-MDR1 (Papp A-B / B-A results 1.8 / 4 and 5 / 5 10–6 cm/s). PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines. PFK-015 suppresses glucose uptake in cancer cells. Rodent PK studies following IV dosing at 5 mg/kg resulted in a profile with a satisfactory half-life (5.1 hours), exposure (AUCinf 1804 ng.h/ml), tissue distribution (Vd 20.5 L/kg) and reasonable clearance (46.2 mL/min/kg). Also, pre-clinical efficacy studies of C57Bl/6 mice bearing Lewis Lung Carcinoma (LLC) xenografts demonstrated 80% tumor growth inhibition relative to vehicle control. Finally, micro-PET studies performed on mice bearing LLC tumors showed a significant inhibition of tumor 2-[18F]-fluoro-2-deoxy-glucose uptake. These results support further development of PFK-015 as a novel anti-cancer agent.

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