Home Tools

Torkinib

Catalog No. T2414 CAS 1092351-67-1

Synonyms: PP 242

Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Torkinib, CAS 1092351-67-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 52.00
10 mg	In stock	$ 68.00
25 mg	In stock	$ 97.00
50 mg	In stock	$ 138.00
100 mg	In stock	$ 239.00
200 mg	In stock	$ 355.00
500 mg	In stock	$ 589.00
1 mL * 10 mM (in DMSO)	In stock	$ 57.00

Bulk Inquiry

Select Batch

Purity: 99.23%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).
Targets&IC50	mTOR:8 nM (cell free), mTORC1:30 nM (cell free), mTORC2:58 nM (cell free), p110δ:0.10 μM (cell free)
In vitro	Torkinib (PP242) potently inhibited mTOR (IC50: 8 nM) but was much less active against other PI3-K family members. Testing of this compound against 219 protein kinases revealed remarkable selectivity relative to the protein kinome. In BT549 cells, PP242 inhibited the phosphorylation of Akt, the mTOR substrate p70S6K, and its downstream target S6 [1]. PP242 suppressed growth by > 90%, with low nanomolar potency (GI50: 12 nM). PP242 had greater anti-proliferative potency relative to rapamycin in a panel of solid tumor cell lines carrying either PI3K gain-of-function or PTEN loss-of-function [2].
In vivo	In mouse p190 model, short-term oral dosing with PP242 in a dose-dependent manner significantly reduced leukemic burden in the spleen and bone marrow. In a long-term survival study, oral dosing of PP242 (30 and 60 mg/kg) significantly delayed the onset of leukemia [2]. In fat and liver, PP242 was able to completely inhibit the phosphorylation of Akt at S473 and T308. Surprisingly, PP242 was only partially able to inhibit the phosphorylation of Akt in skeletal muscle and was more effective at inhibiting the phosphorylation of T308 than S473, despite it's ability to fully inhibit the phosphorylation of 4EBP1 and S6 [3].
Kinase Assay	Purified kinase domains were incubated with inhibitors at 2- or 4-fold dilutions over a concentration range of 50 - 0.001 μM or with vehicle (0.1% DMSO) in the presence of 10 μM ATP, 2.5 μCi of γ-32P-ATP and substrate. Reactions were terminated by spotting onto nitrocellulose or phosphocellulose membranes, depending on the substrate; this membrane was then washed 5–6 times to remove unbound radioactivity and dried. Transferred radioactivity was quantitated by phosphorimaging and IC50 values were calculated by fitting the data to a sigmoidal doseresponse using Prism software [1].
Cell Research	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. Absorbance values (490 nm) were normalized to controls and expressed as %MTS conversion. Wells lacking cells but with MTS added was 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 according to the median-effect method as previously described. For proliferation experiments with PC-3, SKOV3, 786-O, and U87 cells, the CellTiter-Glo Luminescent reagent was used following the manufacturer's instructions. Quantitation was performed as mentioned above [2].
Animal Research	Drugs were prepared in 100 μl of vehicle containing 20% DMSO, 40% PEG-400, and 40% saline. Six-wk-old male C57BL/6 mice were fasted overnight prior to drug treatment. PP242 (0.4 mg), rapamycin (0.1 mg), or vehicle alone was injected IP. After 30 min for the rapamycin-treated mouse or 10 min for the PP242 and vehicle-treated mice, 250 mU of insulin in 100 μl of saline was injected IP. 15 min after the insulin injection, the mice were killed by CO2 asphyxiation followed by cervical dislocation. Tissues were harvested and frozen on liquid nitrogen in 200 μl of cap lysis buffer. The frozen tissue was thawed on ice, manually disrupted with a mortar and pestle, and then further processed with a micro tissue-homogenizer. The protein concentration of the cleared lysate was measured by Bradford assay and 5–10 μg of protein was analyzed by Western blot as described above [3].

Synonyms	PP 242
Molecular Weight	308.34
Formula	C16H16N6O
CAS No.	1092351-67-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 7.7 mg/mL (25 mM)

References and Literature

1. Apsel B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. 2. Janes MR, et al. Effective and selective targeting of leukemia cells using a TORC1/2 kinase inhibitor. Nat Med. 2010 Feb;16(2):205-13. 3. Feldman ME, et al. Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2. PLoS Biol. 2009 Feb 10;7(2):e38.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Kinase Inhibitor Library Antioxidant Compound Library Anti-Cancer Metabolism Compound Library Neural Regeneration Compound Library Neuronal Differentiation Compound Library Anti-Aging Compound Library Autophagy Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

CWI1-2 Linalool KT5823 AT7519 Hydrochloride Demethylzeylasteral D-Pantothenic acid hemicalcium salt RIPGBM Adarotene

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Torkinib 1092351-67-1 Apoptosis Autophagy PI3K/Akt/mTOR signaling Mitophagy PI3K mTOR Mammalian target of Rapamycin PP-242 PP242 inhibit Mitochondrial Autophagy PP 242 Inhibitor inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.