Product Name

Fasnall benzenesulfonate salt

General description

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

Synonym

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-

Purity

≥98.0%(HPLC)

CAS Number

929978-58-5 (free base)

Formula

C¹⁹H²²N⁴S · C⁶H⁵SO³H

Molecular Weight

496.64

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White to beige Solid

Solubility(25℃)

DMSO

≥5mg/mL

l  Biological Information

Biochem/Physiol   Actions

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  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov