所有图片(1)
别名:
5,6-Dimethyl-N-[1-(phenylmethyl)-3-pyrrolidinyl]thieno[2,3-d]pyrimidin-4-amine benzenesulfonate, N-(1-Benzylpyrrolidin-3-yl)-5,6-dimethylthieno[2,3-d] pyrimidin-4-amine benzenesulfonate
经验公式（希尔记法）:
C19H22N4S · C6H5SO3H
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质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
white to beige
溶解性
DMSO: 10 mg/mL, clear
储存温度
2-8°C
SMILES字符串
CC(S1)=C(C)C2=C1N=CN=C2NC3CN(CC4=CC=CC=C4)CC3.O=S(C5=CC=CC=C5)(O)=O
应用
Fasnall benzenesulfonate salt has been used as a fatty acid synthase inhibitor to test its effect on hypoxic U87 MG cells in cell viability assay and lipid droplet formation assay.
生化/生理作用
Fasnall is a fatty acid synthase (FASN or FAS) inhibitor (IC50 = 3.71 ?M by cell-free assay with 200 μM NADPH; IC50 = 147 and 213 nM against acetate and glucose lipids incorporation in HepG2 cells) composed of two enantiomers (HS-79 and HS-80) that selectively target FASN co-factor nucleotide-binding sites without affecting ACC, ZipK, AMPKα, AMPKγ, TRAP1, HSP70, NS5, IRAK2 nucleotide binding or the ATP-binding activity of BT474 cellular proteins. Fasnall is shown to completely block the proliferation in multiple breast cancer cultures at 50 μM as a result of apoptosis induction with much reduced cytotoxicity than C75 toward the non-tumorigenic cell line MCF10A. When administered via i.p. injection, Fasnall is efficacious in prolonging the survival of MMTV-Neu mice by effectively suppressing mammary adenocarcinoma tumor progression (15 mg/kg dosed alone twice weekly or 50 mg/kg dosed with carboplatin once weekly).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
Raffaele Nicastro et al.
Nature cell biology, 25(9), 1303-1318 (2023-08-11)
Cell growth is regulated by the mammalian/mechanistic target of rapamycin complex 1 (mTORC1), which functions both as a nutrient sensor and a master controller of virtually all biosynthetic pathways. This ensures that cells are metabolically active only when conditions are
Anna Barkovskaya et al.
Molecular oncology, 15(8), 2026-2045 (2021-03-25)
Cellular phenotype plasticity between the epithelial and mesenchymal states has been linked to metastasis and heterogeneous responses to cancer therapy, and remains a challenge for the treatment of triple-negative breast cancer (TNBC). Here, we used isogenic human breast epithelial cell
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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