产品名称

Fasnall benzenesulfonate salt

一般描述

Fasnall is a fatty acid synthase (FASN or FAS) inhibitor.

别称

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-

纯 度

≥98.0%(HPLC)

CAS NO.

929978-58-5 (free base)

分子式

C¹⁹H²²N⁴S · C⁶H⁵SO³H

分子量

496.64

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至米色固体

溶解性(25℃)

DMSO

≥5mg/mL

l  生物学信息

生物活性/药理作用

Fasnall is a fatty acid synthase (FASN or FAS) inhibitor (IC₅₀ = 3.71 nM 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).

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.  https://www.ncbi.nlm.nih.gov