PF 05212384

Cat. No. 4823

PF 05212384 C32H41N9O4 [1197160-78-3]

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Alternative Names: PKI-587, Gedatolisib

Chemical Name: N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)phenyl]urea

Biological Activity

Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC50 values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC50 >10 μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC50 < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
615.73
Formula:
C32H41N9O4
Solubility:
Soluble to 5 mM in DMSO with gentle warming
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1197160-78-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Mallon et al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193. PMID: 21325073.

Venkatesan et al (2010) Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor. J.Med.Chem. 53 2636. PMID: 20166697.

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Keywords: PF 05212384, supplier, PF05212384, antitumor, antitumour, PI3-K, phosphoinositide, 3-kinases, mTOR, mammalian, target, of, rapamycin, inhibitors, inhibits, PKI587, Pfizer, Tocris Bioscience, PI 3-kinase Inhibitor products

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