For research use only. Not for therapeutic Use.
P529（Cat No.:I005454）is a potent and selective inhibitor of fibroblast growth factor receptor 1 (FGFR1), a receptor tyrosine kinase involved in cell growth, differentiation, and angiogenesis. By inhibiting FGFR1, P529 effectively blocks downstream signaling pathways such as MAPK/ERK and PI3K/Akt, leading to reduced cell proliferation and migration. P529 is used in cancer research to explore FGFR1’s role in tumor growth and its potential as a therapeutic target, particularly in cancers driven by aberrant FGFR signaling. It also serves as a valuable tool for studying FGFR1-related signaling in other physiological processes.
| Catalog Number | I005454 |
| CAS Number | 914913-88-5 |
| Synonyms | P529 |
| Molecular Formula | C₂₄H₂₂O₆ |
| Purity | ≥95% |
| Target | Akt |
| Solubility | DMSO: ≤ 20.5 mg/mL |
| Storage | -20°C |
| IC50 | < 35 uM (GI50, NCI-60 cell lines) |
| IUPAC Name | 8-(1-hydroxyethyl)-2-methoxy-3-[(4-methoxyphenyl)methoxy]benzo[c]chromen-6-one |
| InChI | 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 |
| InChIKey | YEAHTLOYHVWAKW-UHFFFAOYSA-N |
| SMILES | CC(C1=CC2=C(C=C1)C3=CC(=C(C=C3OC2=O)OCC4=CC=C(C=C4)OC)OC)O |
| Reference | </br>1:Torc1/Torc2 inhibitor, Palomid 529, enhances radiation response modulating CRM1-mediated survivin function and delaying DNA repair in prostate cancer models. Gravina GL, Marampon F, Sherris D, Vittorini F, Di Cesare E, Tombolini V, Lenzi A, Jannini EA, Festuccia C.Prostate. 2014 Jun;74(8):852-68. doi: 10.1002/pros.22804. Epub 2014 Apr 8. PMID: 24715588 </br>2:Subconjunctival Palomid 529 in the treatment of neovascular age-related macular degeneration. Dalal M, Jacobs-El N, Nicholson B, Tuo J, Chew E, Chan CC, Nussenblatt R, Ferris F, Meyerle C.Graefes Arch Clin Exp Ophthalmol. 2013 Dec;251(12):2705-9. doi: 10.1007/s00417-013-2375-7. Epub 2013 May 21. PMID: 23689994 Free PMC Article</br>3:Dual mTORC1 and mTORC2 inhibitor Palomid 529 penetrates the blood-brain barrier without restriction by ABCB1 and ABCG2. Lin F, Buil L, Sherris D, Beijnen JH, van Tellingen O.Int J Cancer. 2013 Sep 1;133(5):1222-33. doi: 10.1002/ijc.28126. Epub 2013 Apr 1. PMID: 23436212 Free Article</br>4: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. Lin F, Sherris D, Beijnen JH, Van Tellingen O.J Chromatogr B Analyt Technol Biomed Life Sci. 2011 Dec 15;879(32):3823-31. doi: 10.1016/j.jchromb.2011.10.028. Epub 2011 Oct 29. PMID: 22100549 </br>5:The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel and cisplatin in aggressive and hormone-refractory prostate cancer cells. Gravina GL, Marampon F, Petini F, Biordi L, Sherris D, Jannini EA, Tombolini V, Festuccia C.Endocr Relat Cancer. 2011 Jul 1;18(4):385-400. doi: 10.1530/ERC-11-0045. Print 2011 Aug. PMID: 21551258 Free Article</br>6:The novel Akt inhibitor Palomid 529 (P529) enhances the effect of radiotherapy in prostate cancer. Diaz R, Nguewa PA, Diaz-Gonzalez JA, Hamel E, Gonzalez-Moreno O, Catena R, Serrano D, Redrado M, Sherris D, Calvo A.Br J Cancer. 2009 Mar 24;100(6):932-40. doi: 10.1038/sj.bjc.6604938. Epub 2009 Feb 24. PMID: 19240717 Free PMC Article</br>7:Palomid 529, a novel small-molecule drug, is a TORC1/TORC2 inhibitor that reduces tumor growth, tumor angiogenesis, and vascular permeability. Xue Q, Hopkins B, Perruzzi C, Udayakumar D, Sherris D, Benjamin LE.Cancer Res. 2008 Nov 15;68(22):9551-7. doi: 10.1158/0008-5472.CAN-08-2058. PMID: 19010932 Free PMC Article |
