An inhibitor of mTORC1 and mTORC2 formation; inhibits VEGF-driven and bFGF-driven endothelial cell proliferation (IC50s = 20 and 30 nM

Palomid 529 – 25 mg

Brand:
Cayman
CAS:
914913-88-5
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Palomid 529 (P529) is an inhibitor of mammalian target of rapamycin complex (mTORC) formation.{39092} It is a derivative of a non-steroidal estrogen antagonist that has anti-angiogenic and anticancer activity but lacks estrogen receptor binding activity in estrogen binding assays in vitro. Palomid 529 inhibits VEGF-driven and bFGF-driven endothelial cell proliferation (IC50s = 20 and 30 nM, respectively) and reduces VEGF-A-driven phosphorylation of AktS473, an mTORC2 substrate. In vivo, palomid 529 inhibits retinal neovascularization in mice with oxygen-induced retinopathy, a commonly used assay for pathogenic angiogenesis, Ad-VEGF-A-driven angiogenesis, and phosphorylation of AktS473. Palomid 529 has anticancer effects in glioma cancer cells and xenografts via AktS473 signaling downtstream of mTORC.  

 

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Description

An inhibitor of mTORC1 and mTORC2 formation; inhibits VEGF-driven and bFGF-driven endothelial cell proliferation (IC50s = 20 and 30 nM, respectively); reduces VEGF-A-driven phosphorylation of AktS473, an mTORC2 substrate; inhibits retinal neovascularization in mice with oxygen-induced retinopathy, Ad-VEGF-A-driven angiogenesis, and phosphorylation of AktS473 in vivo; has anticancer effects in glioma cancer cells and xenografts via AktS473 signaling downtstream of mTORC,

Formal name: 8-(1-hydroxyethyl)-2-methoxy-3-[(4-methoxyphenyl)methoxy]-6H-dibenzo[b,d]pyran-6-one

Synonyms:  P529|RES-529|SG 00529

Molecular weight: 406.4

CAS: 914913-88-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling

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