SML3145

PFK-158

≥98% (HPLC)

• 別名: (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
• 実験式（ヒル表記法）: C₁₈H₁₁F₃N₂O
• CAS番号: 1462249-75-7
• 分子量: 328.29
• MDL番号: MFCD28386154
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear (warmed)
• 保管温度: 2-8°C
• SMILES記法: 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+
• InChI Key: IAJOMYABKVAZCN-AATRIKPKSA-N

詳細

生物化学的／生理学的作用

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.).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable