Name: Fasnall benzenesulfonate
Rating: 5 (10 reviews)

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HIT ID:HIT217659664
Cas No:
常用名:Fasnall benzenesulfonate
IUPAC:1-benzyl-N-{5,6-dimethylthieno[2,3-d]pyrimidin-4-yl}pyrrolidin-3-amine; benzenesulfonic acid
IUPAC:1-benzyl-N-{5,6-dimethylthieno[2,3-d]pyrimidin-4-yl}pyrrolidin-3-amine; benzenesulfonic acid
InChI key:KLKWHGQIUKBXKT-UHFFFAOYSA-N

分子式:C25H28N4O3S2
分子量:496.64
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:OS(=O)(=O)c1ccccc1.Cc1sc2ncnc(NC3CCN(Cc4ccccc4)C3)c2c1C
SMILES:OS(=O)(=O)c1ccccc1.Cc1sc2ncnc(NC3CCN(Cc4ccccc4)C3)c2c1C

Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.

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