[CAS NO. 944808-88-2] CAY10566
PRODUCTS SPECIFICATIONS [944808-88-2]
DESCRIPTION [944808-88-2]
Overview
| MDL | MFCD11976899 |
|---|---|
| Molecular Weight | 389.81 |
| Molecular Formula | C18H17ClFN5O2 |
| SMILES | CC1=NN=C(C2=NN=C(N3CCC(OC4=CC(F)=CC=C4Cl)CC3)C=C2)O1 |
4 Publications Citing Use of MCE
Summary
CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 ( SCD1 ) inhibitor with IC 50 s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC 50 =7.9 nM or 6.8 nM) [1] [2] .
IC50 & Target
IC50: 4.5 nM (SCD1 in mouse), 26 nM (SCD1 in human) [2]
In Vitro
CAY10566 (0.0001-10 μM; 24 hours) concentration-dependently decreases Swiss 3T3 cell proliferation [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay [3]
| 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. |
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) [4] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 64.13 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5654 mL | 12.8268 mL | 25.6535 mL |
| 5 mM | 0.5131 mL | 2.5654 mL | 5.1307 mL |
| 10 mM | 0.2565 mL | 1.2827 mL | 2.5654 mL |
References
- [1] Masuda M, et al. Activating transcription factor 4 regulates stearate-induced vascular calcification. J Lipid Res. 2012 Aug;53(8):1543-52.
- [2] Liu G, et al. Discovery of potent, selective, orally bioavailable stearoyl-CoA desaturase 1 inhibitors. J Med Chem. 2007 Jun 28;50(13):3086-100.
- [3] Koeberle A, et al. Palmitoleate is a mitogen, formed upon stimulation with growth factors, and converted to palmitoleoyl-phosphatidylinositol. J Biol Chem. 2012 Aug 3;287(32):27244-54.
- [4] Kamphorst JJ, et al. Hypoxic and Ras-transformed cells support growth by scavenging unsaturated fatty acids from lysophospholipids. Proc Natl Acad Sci U S A. 2013 May 28;110(22):8882-7.