Free shipping on all orders over $ 500


Cat. No. M1981
PP242 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 70 In stock
50mg USD 220 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

PP242 is a first selective inhibitor that targets ATP domain of mTOR. PP242 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). PP242 induced ERK activation in MM cell lines as well as primary cells. PP242 could also inhibit phosphorylation of AKT on serine 473, a TORC2 substrate, while rapamycin was ineffective. PP242 was more effective than rapamycin in achieving cytoreduction and apoptosis in MM cells. In addition, PP242 was an effective agent against primary MM cells in vitro and growth of 8226 cells in mice. PP242 inhibits both S6K and 4EBP1 phosphorylation; activity causes a decrease in cap-dependent protein translation.

Customer Product Validations & Biological Datas
Source Oncotarget (2015). Figure 1. PP242
Method MTT test
Cell Lines Eras cells
Concentrations 1500 nM
Incubation Time 24 h
Results So, after 24 h treatment with pp242, MTT test reveals a sharp drop in cell viability (up to 90%) that is characteristic for dying cells.
Cell Experiment
Cell lines PC-3, SKOV3, 786-O, and U87 cells
Preparation method In vitro proliferation and drug combination experiments.
Cells were seeded in triplicate wells of 96-well flat bottom culture plates for 48 hr in the presence of increasing concentrations of indicated inhibitors. Cell viability and median-effect dose affecting growth (GIC50) was determined using the MTS assay (Cell Titer 96 Aqueous One solution cell proliferation assay kit; Promega). Absorbance values (490 nm) were normalized to controls and expressed as %MTS conversion. Wells lacking cells but with MTS added were used as the zero value when normalizing. For drug combination experiments, a range of fixed ratios of inhibitors was used to assess synergy using the combination index (CI) with CalcuSyn software (Biosoft) according to the median-effect method as previously described 2. For proliferation experiments with PC-3, SKOV3, 786-O, and U87 cells, the CellTiter-Glo Luminesecent reagent (Promega) was used following the manufacturer’s instructions. Quantitation was performed as mentioned above.
Concentrations 0~10 μM
Incubation time 48 h
Animal Experiment
Animal models xenograft experiments with human Ph+ leukemia
Formulation PEG400 or 5% NMP, 15% PVP, 80% water
Dosages 60mg/kg once daily
Administration oral
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 308.34
Formula C16H16N6O
CAS Number 1092351-67-1
Purity >99%
Solubility DMSO 56 mg/mL
Storage at -20°C

The PP242 mammalian target of rapamycin (mTOR) inhibitor activates extracellular signal-regulated kinase (ERK) in multiple myeloma cells via a target of rapamycin complex 1 (TORC1)/eukaryotic translation initiation factor 4E (eIF-4E)/RAF pathway and activation is a mechanism of resistance.
Hoang B, et al. J Biol Chem. 2012 Jun 22;287(26):21796-805. PMID: 22556409.

Targeting TORC2 in multiple myeloma with a new mTOR kinase inhibitor.
Hoang B, et al. Blood. 2010 Nov 25;116(22):4560-8. PMID: 20686120.

Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor.
Janes MR, et al. Nat Med. 2010 Feb;16(2):205-13. PMID: 20072130.

Related mTOR Products
LY303511 hydrochloride

LY303511 hydrochloride is a structural analogue of LY294002. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via hydrogen peroxide-mediated mitogen-activated protein kinase activation and up-regulation of death receptors.


MHY1485 is an mTOR activator that potently inhibits autophagy by suppression of fusion between autophagosomes and lysosomes.


CZ415 is a potent ATP-competitive mTOR inhibitor with very good cell permeability.


GNE-477 is a potent and efficacious dual PI3K (IC50=4 nM)/mTOR(Ki=21 nM) inhibitor.


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

Abmole Inhibitor Catalog 2017

Keywords: PP242 supplier, mTOR, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.