Palomid 529 (P529) is a novel potent PI3K/Akt/mTOR inhibitor and shows a potent antiproliferative activity in the NCI-60 cell lines panel, with growth inhibitory 50 (GI50) <35 μM. Palomid 529 (P529), which inhibits the TORC1 and TORC2 complexes and shows both inhibition of Akt signaling and mTOR signaling similarly in tumor and vasculature. Palomid 529 (P529) inhibited both VEGF-driven (IC50 = 20 nM) and bFGF-driven (IC50 = 30 nM) endothelial cell proliferation and retained the ability to induce endothelial cell apoptosis.
|Preparation method||Human umbilical vascular endothelial cell proliferation.
The proliferation assay was carried out by seeding the HUVECs in 96-well plates at a density of 1,000 per well in complete medium. Following a 24-h plating period, the cells were starved for 24 h in 0.5% serum before being treated with P529 in the presence of 10 ng/mL basic fibroblast growth factor (bFGF) or VEGF in complete medium. After 48 h, cell number was determined using a colorimetric method as described by the supplier (Promega). The results were expressed as the percentage of the maximal bFGF or VEGF response in the absence of P529. Nonproliferating endothelial cells were assayed by growing HUVECs to quiescence in 96-well plates and treating with P529 for 48 h. Initially, 5,000 cells per well were seeded and confluence was achieved the next day. The plates were incubated for another 24 h to ensure growth arrest before treatment with P529. Cell number was determined as outlined above.
|Incubation time||48 h|
|Animal models||U87 glioma xenograft in Four- to 6-wk-old female nude mice|
|Dosages||50 mg and 25mg/kg/2 d, for 1 wk|
|Solubility (25°C)||DMSO 30 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Lin F et al. J Chromatogr B Analyt Technol Biomed Life Sci. High-performance liquid chromatography analysis of a novel small-molecule, anti-cancer drug, Palomid 529, in human and mouse plasma and in mouse tissue homogenates.
 Gravina GL et al. Endocr Relat Cancer. The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel and cisplatin in aggressive and hormone-refractory prostate cancer cells.
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