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

A939572被用于诱导人类多能干细胞(hPSCs)的细胞死亡，同时也用于体外抑制人类非小细胞肺癌H1299细胞的增殖[1][2]。

无毛裸鼠携带A498 ccRCC异种移植物，经过四周的治疗，分别使用A939572和Tem单独或联合处理，期间测量肿瘤体积(mm3)。A939572和Tem单药治疗产生了类似的生长反应，与安慰剂对照组相比，肿瘤体积大约减少了20-30%，这种减少在研究结束时达到统计学意义，且仅在治疗的最后一周观察到。联合治疗组在研究结束时肿瘤体积减少了60%以上（与安慰剂对照组相比），在治疗约1周后记录到显著减少。所有动物在治疗过程中体重保持健康，然而，在治疗的第一周后，A939572和联合治疗组的动物出现了增加的眨眼频率和轻微的眼部粘膜分泌物[3]。

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].