Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C24H22O6 |
| Molecular Weight | 406.4279 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(COC2=CC3=C(C=C2OC)C4=C(C=C(C=C4)C(C)O)C(=O)O3)C=C1
InChI
InChIKey=YEAHTLOYHVWAKW-UHFFFAOYSA-N
InChI=1S/C24H22O6/c1-14(25)16-6-9-18-19-11-22(28-3)23(12-21(19)30-24(26)20(18)10-16)29-13-15-4-7-17(27-2)8-5-15/h4-12,14,25H,13H2,1-3H3
| Molecular Formula | C24H22O6 |
| Molecular Weight | 406.4279 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
RES-529 (previously named Palomid 529, P529) is a phosphoinositide 3-kinase (PI3K)/AKT/mechanistic target of rapamycin (mTOR) pathway inhibitor that interferes with the pathway through both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2) dissociation. P529 inhibits tumor growth, angiogenesis, and vascular permeability. It retains the beneficial aspects of tumor vascular normalization that rapamycin boasts. This compound is currently being developed in oncology and ophthalmology. The oncology focus is for the treatment of glioblastoma, where it has received orphan designation by the US Food and Drug Administration, and prostate cancer.
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23436212
Curator's Comment: Palomid 529 penetrates the blood-brain barrier in mice. No human data available.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel and cisplatin in aggressive and hormone-refractory prostate cancer cells. | 2011-08 |
|
| The novel Akt inhibitor Palomid 529 (P529) enhances the effect of radiotherapy in prostate cancer. | 2009-03-24 |
|
| Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability. | 2008-11-15 |
Sample Use Guides
Five participants with neovascular age-related macular degeneration that were refractory to intravitreal anti-vascular endothelial growth factor (VEGF) received three serial monthly subconjunctival doses of 1.9 mg Palomid 529.
Mice were treated s.c. with 20 mg/kg Palomid 529 every 3 days.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19240717
Palomid 529 showed a potent antiproliferative activity in the NCI-60 cell lines panel, with growth inhibitory 50 (GI50) <35 microM.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:59:47 GMT 2025
by
admin
on
Mon Mar 31 18:59:47 GMT 2025
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| Record UNII |
XV9409EWG4
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| Record Status |
Validated (UNII)
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| Record Version |
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FDA ORPHAN DRUG |
463714
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