A ring-opened analog of wortmannin that potently and irreversible inhibits PI3K (IC50 = 0.1-88 nM); less potently blocks the activity of mTOR (IC50 = 3.1 µM); exhibits single agent in vivo anti-tumor activity and increases the anti-tumor effects of cisplatin and radiation treatment

PX 866 – 1 mg

Brand:
Cayman
CAS:
502632-66-8
Storage:
-20
UN-No:
Non-Hazardous - /

PX 866 is a ring-opened analog of wortmannin (Item No. 10010591) that potently and irreversibly inhibits PI3K (IC50 = 0.1-88 nM).{24458,18123} It less potently blocks the activity of mammalian target of rapamycin (mTOR, IC50 = 3.1 µM).{18123} PX 866 exhibits single agent in vivo anti-tumor activity and increases the anti-tumor effects of cisplatin and radiation treatment.{24458,24459} In cancer cells grown in three-dimensional cultures, PX 866 reduces cell growth and motility without causing cytotoxicity.{24457} Consistent with having cytostatic effects, PX 866 dosing is associated with prolonged stable disease in cancer patients.{24460}  

 

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Description

A ring-opened analog of wortmannin that potently and irreversible inhibits PI3K (IC50 = 0.1-88 nM); less potently blocks the activity of mTOR (IC50 = 3.1 µM); exhibits single agent in vivo anti-tumor activity and increases the anti-tumor effects of cisplatin and radiation treatment

Formal name: (1E,4S,4aR,5R,6aS,9aR)-5-(acetyloxy)-1-[(di-2-propen-1-ylamino)methylene]-4,4a,5,6,6a,8,9,9a-octahydro-11-hydroxy-4-(methoxymethyl)-4a,6a-dimethyl-cyclopenta[5,6]naphtho[1,2-c]pyran-2,7,10(1H)-trione

Synonyms: 

Molecular weight: 525.6

CAS: 502632-66-8

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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