CAY10566

Cas No.:	944808-88-2
Chemical Name:	3-[4-(2-chloro-5-fluorophenoxy)-1-piperidinyl]-6-(5-methyl-1,3,4-oxadiazol-2-yl)-pyridazine
Synonyms:	CAY10566; CAY-10566; CAY 10566;
SMILES:	CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1
Formula:	C18H17ClFN5O2
M.Wt:	389.82

Description:	CAY10566 is a stearoyl-CoA desaturase (SCD) inhibitor.
In Vivo:	After establishment of palpable tumors, the mice are treated with vehicle or SCD1 inhibitor (2.5 mg/kg CAY10566 orally twice daily). The effect of SCD1 inhibition on the Akt-driven tumors is greater than on the Ras-driven tumors, with the mean tumor volume at day 13 or 14 post therapy, relative to untreated tumors, 0.5±0.04 and 0.67±0.05 respectively (P=0.01 for Ras-Akt comparison, by two-tailed t test)[2].
In Vitro:	Treatment with specific SCD inhibitor CAY10566 dose-dependently reduces SCD activity in MOVAS-1 cells resulting in a significant increase in endoplasmic reticulum (ER) stearate levels. SCD inhibition by CAY10566 treatment induces mineralization and osteoblastic differentiation of MOVAS-1 cells. Along with induction of vascular calcification, CAY10566 dose-dependently induces total ATF4, p-ATF4, and p-eIF2α protein expression. ATF4 mRNA, CHOP protein, CHOP mRNA, and sXBP-1 mRNA levels are also highly and dose-dependently induced by CAY10566 treatment. Phosphorylated PKR-like endoplasmic reticulum kinase (PERK) levels are increased by 15.7-fold at 2 h of CAY10566 treatment, whereas p-eIF2α levels are transiently increased by 1.91-fold at 6 h of CAY10566 treatment. The expressions of ATF4, CHOP, and sXBP mRNA are induced up to 96 h of 300 nM CAY10566 treatment[1].