SML3145

PFK-158

≥98% (HPLC)

• Synonym(s): (2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one, (E)-1-(Pyridyn-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one, PFK 158, PFK158
• Empirical Formula (Hill Notation): C₁₈H₁₁F₃N₂O
• CAS Number: 1462249-75-7
• Molecular Weight: 328.29
• MDL number: MFCD28386154
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (warmed)
• storage temp.: 2-8°C
• SMILES string: O=C(/C=C/C1=NC2=C(C=CC(C(F)(F)F)=C2)C=C1)C3=CC=NC=C3

Description

Biochem/physiol Actions

PFK158 is a 3PO analog with improved PFKFB3 inhibitory potency (cell-free IC50 = 137 nM; Jurkat cellular IC50 = 1.62 μM/PFKFB3 activity, 847 nM/2-deoxyglucose uptake, 328 nM/toxicity) and pharmacokinetic properties. PFK158 markedly sensitizes BRAF(V600E)-positive A375 melanoma cells to apoptosis induction by vemurafenib in cultures and causes ~80% growth inhibition in several murine models of human-derived tumors in vivo (60 mg/kg qod. ip.).

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable