Catalog No.S2218
4.5 5 11 Product Citations

PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.

Price Stock Quantity  
In DMSO USD 91 In stock
USD 70 In stock
USD 120 In stock
USD 370 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

PP242 Chemical Structure

PP242 Chemical Structure
Molecular Weight: 308.34

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

PP242 is available in the following compound libraries:

mTOR Inhibitors with Unique Features

Product Information

  • Compare mTOR Inhibitors
    Compare mTOR Products
  • Research Area
  • Inhibition Profile
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description PP242 is a selective mTOR inhibitor with IC50 of 8 nM; targets both mTOR complexes with >10- and 100-fold selectivity for mTOR than PI3Kδ or PI3Kα/β/γ, respectively.
Targets mTOR [1] p110δ [1] DNA-PK [1] PDGFR [1] Hck [1]

   View More

IC50 8 nM 0.10 μM 0.41 μM 0.41 μM 1.2 μM
In vitro PP242 exhibits potent selectivity for mTOR over other PI3K family kinases such as p110α, p110β, p110γ, p110δ, and DNA-PK with IC50 of 1.96 μM, 2.2 μM, 1.27 μM, 0.102 μM, and 0.408 μM, respectively. PP242 displays some inhibitory activity against Ret, PKCα, PKCβ, and JAK2, while exhibits remarkable selectivity against 215 other protein kinases. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2. In BT549 cells, PP242 treatment (0.04-10 μM) inhibits the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 in a dose-dependent manner. [1] PP242 potently inhibits PKCα with IC50 of 49 nM. Low concentrations of PP242 inhibit the phosphorylation of Akt S473 and higher concentrations partially inhibit Akt T308-P in addition to S473-P. As PP242 is a more effective mTORC1 inhibitor than rapamycin, PP242 inhibits the proliferation of primary MEFs, and the phosphorylation of 4EBP1 at T36/45 and S65, more potently than rapamycin. PP242 but not rapamycin potently inhibits cap-dependent translation, by causing a higher level of binding between 4EBP1 and eIF4E than rapamycin. [2] PP242 potently inhibits the proliferation of p190-transformed murine BM, SUP-B15, and K562 cells with GI50 of 12 nM, 90 nM, and 85 nM, respectively. PP242 also inhibits the growth of solid tumor cell lines such as SKOV3, PC3, 786-O, and U87 with GI50 of 0.49 μM, 0.19 μM, 2.13 μM, and 1.57 μM, respectively. [3] PP242 is also more effective than rapamycin in achieving cytoreduction and apoptosis in multiple myeloma (MM) cells. [4]
In vivo Administration of PP242 is able to completely inhibit the phosphorylation of Akt at S473 and T308 in fat and liver of mice. PP242 only partially inhibits the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite able to fully inhibit the phosphorylation of 4EBP1 and S6. [2] Oral administration PP242 potently delays the leukemia onset in the mice model, and induces leukemia regression by inhibiting mTORC2 and mTORC1 activation that correlates with loss in cell size. [3] PP242 treatment potently inhibits the growth of 8226 cells in mice. [4]
Features One of the first selective inhibitors that targets ATP domain of mTOR.

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro mTOR (FRAP1) kinase assay Recombinant mTOR is incubated with PP242 at 2-fold dilutions over a concentration range of 50-0.001 μM in an assay containing 50 mM HEPES, pH 7.5, 1 mM EGTA, 10 mM MgCl2, 0.01% Tween, 10 μM ATP (2.5 μCi of γ-32P-ATP), and 3 μg/mL BSA. Rat recombinant PHAS-1/4EBP1 (2 mg/mL) is used as a substrate. Reactions are terminated by spotting onto nitrocellulose, which is washed with 1 M NaCl/1% phosphoric acid (approximately 6 times, 5-10 minutes each). Sheets are dried and the transferred radioactivity quantitated by phosphorimaging. IC50 value is calculated by fitting the data to a sigmoidal dose-response curve using the Prism software package.

Cell Assay: [2]

Cell lines MEFs
Concentrations Dissolved in DMSO, final concentrations ~10 μM
Incubation Time 72 hours
Method Cells are treated with increasing concentrations of PP242 for 72 hours in 96-well plates. After 72 hours of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 hours, the florescence intensity in each well is measured using a top-reading florescent plate reader with excitation at 530 nm and emission at 590 nm.

Animal Study: [3]

Animal Models Syngeneic (Balbc/J) mice with mouse p190-transformed BM cells to initiate leukemia, and female NSG mice injected (i.v.) with SUP-B15ffLuc cells or human Ph+ leukemia
Formulation Dissolved in PEG400 (Carbowax polyethylene glycol)
Dosages ~60 mg/kg/day
Administration Oral gavage
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Apsel B, et al. Nat Chem Biol, 2008, 4(11), 691-699.

[2] Feldman ME, et al. PLoS Biol, 2009, 7(2), 0371-0383.

view more

Chemical Information

Download PP242 SDF
Molecular Weight (MW) 308.34


CAS No. 1092351-67-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Solubility (25°C) * In vitro DMSO 62 mg/mL (201 mM)
Water <1 mg/mL (<1 mM)
Ethanol 18 mg/mL (58 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 2-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-1H-indol-5-ol

Research Area

Customer Reviews (2)

Click to enlarge
Source Dr. Zhang of Tianjin Medical University. PP242 purchased from Selleck
Method Western blot
Cell Lines A549 cells
Concentrations 0-10 μM
Incubation Time 24 h
Results PP242 treatment resulted in a reduction of AKT-473 phosphorylation in A549 cells.

Click to enlarge
Source PP242 purchased from Selleck
Method Western Blot
Cell Lines HeLa cells
Concentrations 0/5/50/500/5000 nM
Incubation Time 24 h

Product Citations (11)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related mTOR Products

  • XL388

    XL388 is a highly potent, selective, ATP-competitive inhibitor of mTOR with IC50 of 9.9 nM, 1000-fold selectivity over the closely related PI3K kinases.

  • Zotarolimus(ABT-578)

    Zotarolimus (ABT-578) is an analogue of rapamycin, and inhibits FKBP-12 binding with IC50 of 2.8 nM.

    Features:Zotarolimus has a shorter in vivo half-life and is also demonstrated in rats to have less potent systemic immunosuppression than rapamycin.

  • Dorsomorphin 2HCl

    Dorsomorphin is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Also inhibits BMP type I receptor.

  • Rapamycin (Sirolimus)

    Rapamycin (Sirolimus, AY-22989, WY-090217) is a specific mTOR inhibitor with IC50 of ~0.1 nM.

  • Everolimus (RAD001)

    Everolimus (RAD001) is an mTOR inhibitor of FKBP12 with IC50 of 1.6-2.4 nM.

  • AZD8055

    AZD8055 is a novel ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (∼1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1.

    Features:First drug to inhibit both types of mTOR protein.

  • Torin 1

    Torin 1 is a potent inhibitor of mTORC1/2 with IC50 of 2 nM/10 nM; exhibits 1000-fold selectivity for mTOR than PI3K.

  • INK 128 (MLN0128)

    INK 128 (MLN0128) is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms, superior in blocking mTORC1/2 and sensitive to pro-invasion genes (vs Rapamycin). Phase 1.

  • Temsirolimus (CCI-779, NSC 683864)

    Temsirolimus (CCI-779) is a specific mTOR inhibitor with IC50 of 1.76 μM.

  • KU-0063794

    KU-0063794 is a potent and highly specific dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of ~10 nM; no effect on PI3Ks.

Recently Viewed Items

Tags: buy PP242 | PP242 supplier | purchase PP242 | PP242 cost | PP242 manufacturer | order PP242 | PP242 distributor
Contact Us