PP 242

Key Product Details

Product Description

PP 242 is an 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 cFLIP_S and augments TRAIL-induced apoptosis of cancer cells. PP 242 also inhibits oncogenic K-Ras and PI 3-K induced lipogenesis in breast cancer cells.

Product Specifications for PP 242

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

Solubility

Preparing Stock Solutions for PP 242

The following data is based on the product molecular weight 308.34.

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
0.25 mM	12.97 mL	64.86 mL	129.73 mL
1.25 mM	2.59 mL	12.97 mL	25.95 mL
2.5 mM	1.30 mL	6.49 mL	12.97 mL
12.5 mM	0.26 mL	1.30 mL	2.59 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 66 publications citing the usage of this product.

• Ricoult Oncogenic PI3K and K-Ras stimulate de novo lipid synthesis through mTORC1 and SREBP. Oncogene 2016 PMID: 26028026
• Zhao mTOR complex 2 is involved in regulation of Cbl-dependent c-FLIP regulation and sensitivity of TRAIL-induced apoptosis. Cancer Res. 2013 PMID: 23319802
• Janes Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat.Med. 2010 PMID: 20072130
• Feldman Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 2009 PMID: 19209957
• Apsel Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat.Chem.Biol. 2008 PMID: 18849971

Product Documents for PP 242