PFK-158 ≥98% (HPLC)

Sinônimo(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

Sobre este item

Fórmula empírica (Notação de Hill):

C₁₈H₁₁F₃N₂O

Número CAS:

1462249-75-7

Peso molecular:

328.29

Número MDL:

MFCD28386154

Código UNSPSC:

12352200

NACRES:

NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear (warmed)

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

O=C(/C=C/C1=NC2=C(C=CC(C(F)(F)F)=C2)C=C1)C3=CC=NC=C3

InChI

1S/C18H11F3N2O/c19-18(20,21)14-3-1-12-2-4-15(23-16(12)11-14)5-6-17(24)13-7-9-22-10-8-13/h1-11H/b6-5+

chave InChI

IAJOMYABKVAZCN-AATRIKPKSA-N

Ações bioquímicas/fisiológicas

3PO analog with improved PFKFB3 inhibitory potency in vitro and in vivo.

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.).