Molecular Formula | C24H22O6
|
Molar Mass | 406.43 |
Density | 1.280 |
Solubility | DMSO: soluble10mg/mL, clear |
Appearance | powder |
Color | white to beige |
Storage Condition | -20°C |
Use | Palomid 529 (P529) inhibits mTORC1 and mTORC2 complexes, reduces pAktS473, pGSK3βS9 and pS6 phosphorylation, but has no effect on pMAPK and pAktT308 |
In vitro study | Palomid 529 inhibits endothelial cell proliferation and increases apoptosis. Palomid 529 inhibit VEGF-mediated and bFGF-mediated endothelial cell proliferation with IC 50 of 20 nM and 30 nM, respectively. Palomid 529 induces endothelial cell apoptosis and decreases VEGF VEGF-A-driven phosphorylation of pAktS473, pGSK3βS9, and pS6. However, Palomid 529 did not inhibit mitogen-activated protein kinase (pMAPK) phosphorylation or pAktT308 phosphorylation as effectively as it reduced pAktS473 phosphorylation. Palomid529 not only reduces the proliferation of ischemic retina, but also improves the formation of blood vessels in tissues and structures. Palomid 529 showed highly potent antiproliferative activity in lung cancer NCI- 60 cell line with GI50< 35 μm. In addition, Palomid 529 significantly exacerbates radiation-induced antiproliferative effects PC-3 prostate cancer cells. The growth inhibition was concentration-dependent. Doses of 2 and 7 μm resulted in 30 and 60% growth inhibition, respectively. Palomid 529 inhibits radiation-induced p-Akt activation and reduces Bcl-2/Bax ratio in PC-3. Palomid 529 not only inhibits radiation-induced Id-1 and VEGF overexpression but also downregulates radiation-induced MMP-2 and MMP-9. |
In vivo study | Palomid 529 dose-dependently inhibited Ad-VEGF-A-driven angiogenesis, and Palomid 529 inhibited C6V10 glioma growth in nude mice after intragastric administration. The Palomid 529 acts on the AktS473 signal but not on the AktT308 signal. Palomid 529 inhibit tumor growth, angiogenesis, and vascular permeability. Treatment of mice with PC-3 tumors with Palomid 529 reduced tumor growth by 57.1 percent compared to the control group. Palomid 529 potently inhibits Müller cell proliferation, glial scar formation, and photoreceptor cell death in a rabbit retinal detachment (RD) model. In a mouse Brca1 deletion tumor growth model, Palomid 529 significantly inhibited both the Akt and mTOR signaling pathways. |