Biological Activity
ATP-competitive mTORC1/mTORC2 inhibitor (IC50 = 8 nM). Displays selectivity for mTOR over other PI 3K family kinases (IC50 values are 0.102, 0.408, 1.27, 1.96 and 2.2 μM for p110γ, DNA-PK, p110δ, p110α and p110β respectively) and 215 further kinases. Displays modest inhibition of PKCα, JAK2, PKCβI, PKCβII and RET (IC50 values are 0.049, 0.110, 0.185, 0.198 and 0.224 μM respectively). Inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation. Also triggers downregulation of cFLIPS and augments TRAIL-induced apoptosis of cancer cells.
Compound Libraries
PP 242 is also offered as part of the Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 308.34 |
| Formula | C16H16N6O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1092351-67-1 |
| PubChem ID | 25243800 |
| InChI Key | MTICIDWIKCANDD-WYMLVPIESA-N |
| Smiles | OC1=CC2=C(NC(C3=NN(C(C)C)C4=C3C(N)=NC=N4)=C2)C=C1 |
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 | 7.71 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 308.34. 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 | 3.24 mL | 16.22 mL | 32.43 mL |
| 5 mM | 0.65 mL | 3.24 mL | 6.49 mL |
| 10 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.65 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Apsel et al (2008) Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 4 691 PMID: 18849971
Janes et al (2010) Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat.Med. 16 205 PMID: 20072130
Feldman et al (2009) Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 7 371 PMID:
Zhao et al (2013) mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP regulation and sensitivity of TRAIL-induced apoptosis. Cancer Res. 73 1946 PMID: 23319802
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