| Identification | Back Directory | [Name]
Thieno[2,3-d]pyrimidin-4-amine, 5,6-dimethyl-N-[1-(phenylmethyl)-3-pyrrolidinyl]-, compd. with benzenesulfonate (1:1) | [CAS]
2187367-11-7 | [Synonyms]
Thieno[2,3-d]pyrimidin-4-amine, 5,6-dimethyl-N-[1-(phenylmethyl)-3-pyrrolidinyl]-, compd. with benzenesulfonate (1:1) | [Molecular Formula]
C19H22N4S.C6H6O3S |
| Hazard Information | Back Directory | [Description]
Fasnall is an inhibitor of fatty acid synthase (FASN) with an IC50 value of 3.71 μM for the human recombinant enzyme.1 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 response in vivo, increasing the objective response rate of stable disease from 25% for carboplatin alone to 88% for carboplatin with fasnall.
| [References]
1. Alwarawrah, Y., Hughes, P., Loiselle, D., et al. Fasnall, a selective FASN inhibitor, shows potent anti-tumor activity in the MMTV-Neu model of HER2+ breast cancer Cell Chem. Bio. 23(6),678-688(2016). |
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