Fasnall (benzenesulfonate)

Fasnall is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 3.71 µM for the human recombinant enzyme. It inhibits tritiated acetate incorporation into lipids (IC50 = 5.84 µM), increases ceramide accumulation, and induces the formation of lipid droplets in BT474 HER2+ breast cancer cells. Fasnall has antiproliferative activity against non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3 breast cancer cells that directly correlates to the level of FASN expression in vitro. It reduces tumor volume and increases survival in the murine MMTV-Neu model of HER2+ breast cancer. Fasnall also potentiates carboplatin (Cay-13112) response in vivo, increasing the objective response rate of stable disease from 25% for carboplatin alone to 88% for carboplatin with fasnall.Formal Name: 5,6-dimethyl-N-[1-(phenylmethyl)-3-pyrrolidinyl]-thieno[2,3-d]pyrimidin-4-amine, monobenzenesulfonate. CAS Number: 2187367-11-7. Molecular Formula: C19H22N4S . C6H6O3S. Formula Weight: 496.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 212, 279 nm. SMILES: CC1=C(C)SC2=NC=NC(NC3CCN(CC4=CC=CC=C4)C3)=C21.OS(C5=CC=CC=C5)(=O)=O. InChi Code: InChI=1S/C19H22N4S.C6H6O3S/c1-13-14(2)24-19-17(13)18(20-12-21-19)22-16-8-9-23(11-16)10-15-6-4-3-5-7-15,7-10(8,9)6-4-2-1-3-5-6/h3-7,12,16H,8-11H2,1-2H3,(H,20,21,22),1-5H,(H,7,8,9). InChi Key: KLKWHGQIUKBXKT-UHFFFAOYSA-N.