PP 242
Tocris Bioscience, part of Bio-Techne | Catalog # 4257
Dual mTORC1/mTORC2 inhibitor
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 cFLIPS 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
Molecular Weight
308.34
Formula
C16H16N6O
Storage
Store at +4°C
Purity
≥98% (HPLC)
Chemical Name
2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.71 | 25 |
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the 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 Specific Notices for PP 242
For research use only
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