质量水平
检测方案
≥97% (HPLC)
形式
powder
颜色
white to light brown
溶解性
DMSO: 5 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
O=C(C1CC1)N2CC[C@@H](CC(N3C4=CC=C(C5=CC=C(OC=C6)C6=C5)C=C4)=NNC3=O)C2
InChI
1S/C25H24N4O3/c30-24(18-1-2-18)28-11-9-16(15-28)13-23-26-27-25(31)29(23)21-6-3-17(4-7-21)19-5-8-22-20(14-19)10-12-32-22/h3-8,10,12,14,16,18H,1-2,9,11,13,15H2,(H,27,31)/t16-/m0/s1
InChI key
AQTPWCUIYUOEMG-INIZCTEOSA-N
生化/生理作用
GSK2194069 是脂肪酸合酶（FAS）抑制剂。GSK2194069 是 hFAS 的 β-酮酯酰还原酶（KR）活性的有效和特异性抑制剂，整个 hFAS 反应的 IC50 为 7.7±4.1 nM。 FAS 在某些癌症（包括前列腺癌）中上调。 研究发现 GSK2194069 抑制 Nod-SCID-γ 小鼠体内产生的前列腺癌 C42b 细胞异种移植物的肿瘤生长。 在非小细胞肺癌（A549）癌细胞系中也证实了细胞 FAS 抑制作用会减少细胞生长，平均 EC50 为 15±0.5 nM。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
David Weigt et al.
Cell chemical biology, 26(9), 1322-1331 (2019-07-08)
Human cancers require fatty acid synthase (FASN)-dependent de novo long-chain fatty acid synthesis for proliferation. FASN is therefore an attractive drug target, but fast technologies for reliable label-free cellular compound profiling are lacking. Recently, MALDI-mass spectrometry (MALDI-MS) has emerged as
Myriam Cerezo-Magaña et al.
Molecular cancer research : MCR, 19(3), 528-540 (2020-12-09)
As an adaptive response to hypoxic stress, aggressive tumors rewire their metabolic phenotype into increased malignant behavior through extracellular lipid scavenging and storage in lipid droplets (LD). However, the underlying mechanisms and potential lipid source retrieved in the hypoxic tumor
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