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Palomid 529

Cat. No. M1760
Palomid 529 Structure
Synonym:

P529

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 48  USD48 In stock
10mg USD 70  USD70 In stock
50mg USD 230  USD230 In stock
100mg USD 360  USD360 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
Cell lines HUVECs
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.
Concentrations 0~10mM
Incubation time 48 h
Animal Experiment
Animal models U87 glioma xenograft in Four- to 6-wk-old female nude mice
Formulation saline
Dosages 50 mg and 25mg/kg/2 d, for 1 wk
Administration i.p.
Chemical Information
Molecular Weight 406.43
Formula C24H22O6
CAS Number 914913-88-5
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] 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.

[2] 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.

[3] Diaz R et al. Br J Cancer. The novel Akt inhibitor Palomid 529 (P529) enhances the effect of radiotherapy in prostate cancer.

[4] Xue Q et al. Cancer Res. Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability.

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Keywords: Palomid 529, P529 supplier, mTOR, inhibitors, activators


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