A939572 is stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM for mSCD1 and 37 nM for hSCD1.

SCD1 (human):37 nM, SCD1 (mouse):<4 nM

Caki1 and A498 cells were transiently transfected with p5xATF6-GL3 UPR luciferase reporter and pRL-CMV-renilla luciferase plasmid using Lipofectamine2000 (Invitrogen). Cells (DMSO vs. A939572, NT vs. shSCD780) were harvested after 48hrs using Dual Luciferase assay kit per the manufacturer s protocol and luciferase activity was measured using a Veritas Luminometer; reported as relative luminescence[3].

A498 cells were subcutaneously implanted in athymic nu/nu mice at 1×10^6 cells/mouse in 50%Matrigel.?Tumors reached ~50 mm^3 prior to 4wk treatment.?A939572 was re-suspended in strawberry-flavored Kool-Aid in sterilized H2O (0.2g/mL) vehicle at 30mg/kg in a 50μl dose.?Mice were orally fed by using a syringe to administer the 50μl dose twice daily/mouse.?This modified method was found to be effective and less stressful on the mice.?Temsirolimus was solubilized in 30% ethanol/saline and administered via intraperitoneal injection at 10mg/kg in a 50μl dose once every 72hrs/mouse.?Tumor volumes were calculated using the formula and body weight were measured every 3 days[3].

DMSO: 45 mg/mL (116.02 mM), Sonication is recommended.

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.16 mM), Sonication is recommended.