CAY10566

SKU: orb1219589

Description

CAY10566 shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM). CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively..CAY10566 (0.0001-10 μM; 24 hours), concentration-dependently, decreases Swiss 3T3 cell proliferation.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).

Key Properties

• CAS Number: 944808-88-2
• MW: 389.81
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₇ClFN₅O₂
• SMILES: Cc1nnc(o1)-c1ccc(nn1)N1CCC(CC1)Oc1cc(F)ccc1Cl
• Target: Dehydrogenase
• Solubility: DMSO:24 mg/mL (61.57 mM; Need ultrasonic)

Bioactivity

• In Vitro:
  Cell Proliferation Assay Cell line: Swiss 3T3 cells. Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM Incubation time: 24 hours. Result: Swiss 3T3 cell proliferation was concentration-dependently decreased.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Dehydrogenase