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 |
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 3.08 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 615.73. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.62 mL | 8.12 mL | 16.24 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.25 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Mallon et al (2011) Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor. Clin.Cancer Res. 17 3193 PMID: 21325073
Keywords: PF 05212384, supplier, PF05212384, antitumor, antitumour, PI3-K, phosphoinositide, 3-kinases, mTOR, mammalian, target, of, rapamycin, inhibitors, inhibits, PKI587, Pfizer, PKI-587, Gedatolisib, PI, 3-Kinase, mTOR, PI, 3-Kinase, Tocris Bioscience
