SW203668 

SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC₅₀ of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer^[1].

SW203668 is selectively cytotoxic to 4 human NSCLC cell lines (H2122, H460, and 2 others) with IC₅₀ values of 0.022-0.116 μM, and shows no toxicity to 8 other human NSCLC cell lines at concentrations up to 10 μM^[1].
SW203668 inhibits SCD activity in H2122 cell microsomes with an IC₅₀ of 0.054 μM^[1].
SW203668 is activated by CYP4F11 to crosslink and inhibit SCD, conferring cytotoxicity to previously insensitive H1155 NSCLC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SW203668 (6-25 mg/kg; i.p.; once/twice daily; 14-15 days) selectively inhibits growth of CYP4F11-expressing H2122 xenograft tumors in mice at doses that spare sebocyte viability, with 25 mg/kg twice daily showing potent tumor growth inhibition and 20 mg/kg once daily demonstrating significant sebocyte preservation relative to a conventional SCD inhibitor^[1].
SW203668 (6-20 mg/kg; i.p.; once daily; 15 days) spares sebocyte viability in healthy CD-1 mice at daily i.p. doses of 6 mg/kg and 20 mg/kg for 15 days, with 20 mg/kg showing significantly higher sebocyte counts than a conventional SCD inhibitor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

389.47

C₂₂H₁₉N₃O₂S

1673556-40-5

COC1=CC=C2C(SC(NC(C3=CC=C(C=C3)C(C4=CC=CC=C4)N)=O)=N2)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Theodoropoulos PC, et al. Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase. Nat Chem Biol. 2016;12(4):218-225.  [Content Brief]