PF 05212384

Name: PF 05212384
Brand: Tocris Bioscience
SKU: 4823

Tocris Bioscience, part of Bio-Techne | Catalog # 4823

COA / SDS

Potent and selective dual PI 3-K/mTOR inhibitor

Discontinued Product

4823 has been discontinued. View all PI 3-Kinase Inhibitors products.

Key Product Details

Description:	Potent and selective dual PI 3-K/mTOR inhibitor
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
Purity:	≥98% (HPLC)
Molecular Weight:	615.73

View Full Technical Details for PF 05212384

Technical Data
Citations

Biological Activity for PF 05212384

PF 05212384 is a 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 for PF 05212384

M. Wt	615.73
Formula	C₃₂H₄₁N₉O₄
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1197160-78-3
PubChem ID	44516953
InChi Key	DWZAEMINVBZMHQ-UHFFFAOYSA-N
Smiles	O=C(NC5=CC=C(C(N6CCC(N(C)C)CC6)=O)C=C5)NC(C=C4)=CC=C4C1=NC(N2CCOCC2)=NC(N3CCOCC3)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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References for PF 05212384

References are publications that support the biological activity of the product.

Mallon Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 2011 PMID: 21325073
Venkatesan 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. 2010 PMID: 20166697