An inhibitor of FASN
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Fasnall (benzenesulfonate)

Item No. 19957

Technical Information
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
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product 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 (Item No. 13112) response in vivo, increasing the objective response rate of stable disease from 25% for carboplatin alone to 88% for carboplatin with fasnall.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Alwarawrah, Y., Hughes, P., Loiselle, D., et alFasnall, 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).