PF 05212384

Key Product Details

Product Description

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.

Product Specifications for PF 05212384

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

Solubility

Preparing Stock Solutions for PF 05212384

The following data is based on the product molecular weight 615.73.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.05 mM	32.48 mL	162.41 mL	324.82 mL
0.25 mM	6.50 mL	32.48 mL	64.96 mL
0.5 mM	3.25 mL	16.24 mL	32.48 mL
2.5 mM	0.65 mL	3.25 mL	6.50 mL

Calculators

Background References

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

Product Documents for PF 05212384