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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
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
生化/生理作用
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.).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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