PP 242

Name: PP 242
Brand: Tocris Bioscience
SKU: 4257

Tocris Bioscience, part of Bio-Techne | Catalog # 4257

Citations (57)

COA / SDS

Dual mTORC1/mTORC2 inhibitor

Key Product Details

Description:	Dual mTORC1/mTORC2 inhibitor
Chemical Name:	2-[4-Amino-1-(1-methylethyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1H-indol-5-ol
Purity:	≥98% (HPLC)
Molecular Weight:	308.34

View Full Technical Details for PP 242

Technical Data
Citations

Biological Activity for PP 242

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.

Compound Libraries for PP 242

PP 242 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.

Technical Data for PP 242

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for PP 242

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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 will 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

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References for PP 242

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