Art. -Nr.: HY-10474

Torkinib

(Synonyms: PP 242)

30 Cited Publications

Kundenbewertung

Based on 30 publication(s) in Google Scholar

Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC₅₀ of 8 nM. PP242 inhibits both mTORC1 and mTORC2 with IC₅₀s of 30 nM and 58 nM, respectively.

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Reinheit: 99.03%
CAS. Nr.: 1092351-67-1
Formel: C₁₆H₁₆N₆O
Molecular Weight:308.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Torkinib Chemical Structure

CAS. Nr.: 1092351-67-1

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Use of MCE Products

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (30)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC₅₀ of 8 nM^[1]. PP242 inhibits both mTORC1 and mTORC2 with IC₅₀s of 30 nM and 58 nM, respectively^[2].

IC₅₀ & Target^[1]^[2]

mTOR

8 nM (IC₅₀)

mTORC1

30 nM (IC₅₀)

mTORC2

58 nM (IC₅₀)

p110δ

100 nM (IC₅₀)

PDGFR

410 nM (IC₅₀)

DNA-PK

410 nM (IC₅₀)

p110γ

1.3 μM (IC₅₀)

p110α

2 μM (IC₅₀)

p110β

2.2 μM (IC₅₀)

Hck

1.2 μM (IC₅₀)

Scr

1.4 μM (IC₅₀)

VEGFR2

1.5 μM (IC₅₀)

Abl

3.6 μM (IC₅₀)

EphB4

3.4 μM (IC₅₀)

EGFR

4.4 μM (IC₅₀)

Scr(T338I)

5.1 μM (IC₅₀)

Autophagy

Mitophagy

Alle mTOR Isoform-spezifische Produkte anzeigen :

In Vitro

Torkinib (PP 242) potently inhibits mTOR (IC₅₀=8 nM) but is much less active against other PI3K family members. Testing of Torkinib (PP 242) against 219 protein kinases reveals remarkable selectivity relative to the protein kinome: at a concentration 100-fold above its IC₅₀ for mTOR, Torkinib (PP 242) inhibits only one kinase by more than 90% (Ret) and only three by more than 75% (PKCα, PKCβII and JAK2^V617F)^[1]. Torkinib (PP 242) has a dose-dependent effect on proliferation and at higher doses is much more effective than Rapamycin at blocking cell proliferation. The ability of Torkinib (PP 242) to block cell proliferation more efficiently than Rapamycin could be a result of its ability to inhibit mTORC1 and mTORC2, because Rapamycin can only inhibit mTORC1. In SIN1^-/- mouse embryonic fibroblasts (MEFs), Rapamycin is also less effective at blocking cell proliferation than Torkinib. That Torkinib (PP 242) and Rapamycin exhibit very different anti-proliferative effects in SIN1^-/- MEFs suggests that the two compounds differentially affect mTORC1^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In fat and liver, Torkinib (PP 242) is able to completely inhibit the phosphorylation of Akt at S473 and T308, consistent with its effect on these phosphorylation sites observed in cell culture. Surprisingly, Torkinib (PP 242) is only partially able to inhibit the phosphorylation of Akt in skeletal muscle and is more effective at inhibiting the phosphorylation of T308 than S473, despite it's ability to fully inhibit the phosphorylation of 4EBP1 and S6. These results will be confirmed by in vivo dose-response experiments, but, consistent with the partial effect of Torkinib (PP 242) on pAkt in skeletal muscle, a muscle-specific knockout of the integral mTORC2 component rictor resulted in only a partial loss of Akt phosphorylation at S473. These results suggest that a kinase other than mTOR, such as DNA-PK, may contribute to phosphorylation of Akt in muscle^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1092351-67-1
Appearance Solid
Molecular Weight 308.34
Formel C₁₆H₁₆N₆O
Color Light yellow to yellow
SMILES

NC1=C2C(N(N=C2C3=CC4=C(N3)C=CC(O)=C4)C(C)C)=NC=N1
Synonyms

PP 242
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (30)

All Cell Proliferation/Viability AssayWBCell Migration/Invasion AssayFlow CytometryIn Vivo Efficacy StudyHistological Imaging/Staining

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Journal Impact Factor

Cancer Res

Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR. [Abstract]

2013 Apr 15;73(8):2574-86. PMID: 23436801
Theranostics

β-glucan-coupled superparamagnetic iron oxide nanoparticles induce trained immunity to protect mice against sepsis. [Abstract]

2022 Jan 1;12(2):675-688. PMID: 34976207
Acta Pharm Sin B

RICTOR/mTORC2 affects tumorigenesis and therapeutic efficacy of mTOR inhibitors in esophageal squamous cell carcinoma. [Abstract]

2020 Jun;10(6):1004-1019. PMID: 32642408

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

ECa109 cells stably transfected with control shRNA or RICTOR shRNA were treated with RAD001 (10 μmol/L) or Torkinib (PP242, 2 μmol/L) for 48 h, and total proteins were extracted to analysis the expression of RICTOR, p-AKT (Ser473), AKT, p-PRAS40 (Thr246), PRAS40, p-p70S6K and p70S6K by Western blot (n=5).

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

ECa109 and EC9706 cells were treated with Torkinib (PP242) for 24 or 48 h, respectively, and the cell viability was assessed by CCK-8 assay (n = 5).

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

After ECa109 and EC9706 cells were treated with Torkinib (PP242) (0, 1 and 4 μmol/L) for 24 h or at the same concentration (4 μmol/L of PP242) for different time, total proteins were extracted to analyze the expression of p-AKT (Ser473), AKT, p-p70S6K and p70S6K by Western blot (n = 5). The results showed that PP242 decreased the expression of p-AKT (Ser473) and p-p70S6K (Thr389) in dose- and time-dependent manners.

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

ECa109 RICTOR-KD cells or control cells were treated with RAD001 (10 μmol/L) or Torkinib (PP242) (2 μmol/L) for 48 h, and then the cell migration was assessed by transwell migration assay (n = 3). Scale bar = 100 μm.

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

ECa109 RICTOR-KD cells or control cells were treated with RAD001 (20 μmol/L) or Torkinib (PP242) (4 μmol/L) for 48 h, and then cell apoptosis was assessed by flow cytometry (n = 3).

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

ECa109 RICTOR-KD cells or control cells were treated with RAD001 (10 μmol/L) or PP242 (2 μmol/L ) for 48 h, and then the cell cycle were assessed by flow cytometer (n = 3).

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

Stable knockdown of RICTOR inhibited tumor growth and potentiated the antitumor effect of Torkinib (PP242) in nude mice. Nude mice bearing tumors derived from ECa109 RICTOR-KD cells or control cells were treated by Torkinib (PP242) (5 mg/kg every other day, i.p.) for 14 days (n = 5). Tumor growth curves were graphed with the tumor volume of each mouse measured and recorded every day (n = 5).

Torkinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2020 Jun;10(6):1004-1019. [Abstract]

Nude mice bearing tumors derived from ECa109 RICTOR-KD cells or control cells were treated by Torkinib (PP242) (5 mg/kg every other day, i.p.) for 14 days (n = 5). Paraffin-embedded tumor was used to analyze the cell apoptosis as well as livers and kidneys of mice were used to evaluate the potential hepatorenal toxicity by H&E staining (n = 5). Scale bar = 100 μm.
J Exp Clin Cancer Res

The EGFR-HSF1 axis accelerates the tumorigenesis of pancreatic cancer. [Abstract]

2021 Jan 9;40(1):25. PMID: 33422093
Adv Sci (Weinh)

Depletion of Hepatic SREBP2 Protects Against Hypercholesterolemia and Atherosclerosis through the ANGPTL3-LPL Axis. [Abstract]

2025 May;12(18):e2412677. PMID: 40106311
Environ Int

Exploring seasonal dynamics of sea spray aerosol bioactivity: Insights into molecular effects on human bronchial epithelial cells. [Abstract]

2025 Jan:195:109255. PMID: 39787780
Oncogene

Jumonji histone demethylases are therapeutic targets in small cell lung cancer. [Abstract]

2024 Sep;43(38):2885-2899. PMID: 39154123
Curr Biol

Polyploidy in Xenopus lowers metabolic rate by decreasing total cell surface area. [Abstract]

2023 May 8;33(9):1744-1752.e7. PMID: 37080197
Br J Pharmacol

High-throughput screening identifies bazedoxifene as a potential therapeutic for dysferlin-deficient limb girdle muscular dystrophy. [Abstract]

2025 Jul;182(13):2930-2949. PMID: 40108832
Breast Cancer Res

FAK activates AKT-mTOR signaling to promote the growth and progression of MMTV-Wnt1-driven basal-like mammary tumors. [Abstract]

2020 Jun 3;22(1):59. PMID: 32493400
Geroscience

Autophagy revealed as a targetable vulnerability in senescent cells by cell painting phenotypic profiling: a mechanistic study of MCOPPB and related compounds. [Abstract]

2026 Apr 30. PMID: 42062708
Mol Cancer Res

Dual Regulation of Histone Methylation by mTOR Complexes Controls Glioblastoma Tumor Cell Growth via EZH2 and SAM. [Abstract]

2020 Aug;18(8):1142-1152. PMID: 32366675
Mar Drugs

Aerosolizable Marine Phycotoxins and Human Health Effects: In Vitro Support for the Biogenics Hypothesis. [Abstract]

2020 Jan 10;18(1):46. PMID: 31936833
Inflammation

Oroxylin A-induced Trained Immunity Promotes LC3-associated Phagocytosis in Macrophage in Protecting Mice Against Sepsis. [Abstract]

2024 Dec;47(6):2196-2214. PMID: 38739341
Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11:11:580407. PMID: 33343350
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
PLoS Pathog

Manganese is a potent inducer of lysosomal activity that inhibits de novo HBV infection. [Abstract]

2025 Jan 2;21(1):e1012800. PMID: 39746094
Sci Rep

Evaluation of the antitumor effects of PP242 in a colon cancer xenograft mouse model using comprehensive metabolomics and lipidomics. [Abstract]

2020 Oct 16;10(1):17523. PMID: 33067464
J Virol

Tripartite motif 25 inhibits protein aggregate degradation during PRRSV infection by suppressing p62-mediated autophagy. [Abstract]

2024 Nov 19;98(11):e0143724. PMID: 39480084
J Biol Chem

Phosphatases maintain low catalytic activity of SGK1: DNA damage resets the balance in favor of phosphorylation. [Abstract]

2023 Aug;299(8):104941. PMID: 37343701
J Cell Sci

A C-terminal cytoplasmic retention motif and nuclear localization signal regulates nuclear import of TP53INP2. [Abstract]

2025 Dec 15;138(24):jcs264267. PMID: 41368677
ACS Chem Biol

Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. [Abstract]

2012 Jun 15;7(6):982-7. PMID: 22496512
Front Oncol

RAD21 Confers Poor Prognosis and Affects Ovarian Cancer Sensitivity to Poly(ADP-Ribose)Polymerase Inhibitors Through DNA Damage Repair. [Abstract]

2022 Jul 4;12:936550. PMID: 35860572
Mol Biol Rep

mTOR inhibitor PP242 increases antitumor activity of sulforaphane by blocking Akt/mTOR pathway in esophageal squamous cell carcinoma. [Abstract]

2022 Jan;49(1):451-461. PMID: 34731371
Hum Cell

Multi-omics data integration reveals the molecular network of dysregulation IQGAP2-mTOR promotes cell proliferation. [Abstract]

2023 Jul;36(4):1429-1440. PMID: 37154877
Biochem Biophys Res Commun

mTORC2/Akt axis promotes proteotoxic stress and mitochondrial Ca2+ overload during celastrol-induced paraptosis. [Abstract]

2025 Aug 11:781:152474. PMID: 40834605
bioRxiv

Ras-Responsive Element Binding Protein 1 regulates survival of Group 3 medulloblastoma. [Abstract]

2025 Jul 21:2025.07.16.665230. PMID: 40777316
Res Sq

2025 Jul 13.
Ghent University

2021 Oct.
Research Square Preprint

2021 May.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (162.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2432 mL

16.2159 mL

32.4317 mL

5 mM

0.6486 mL

3.2432 mL

6.4863 mL

10 mM

0.3243 mL

1.6216 mL

3.2432 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

Wild-type and SIN1^-/- MEFs are plated in 96-well plates at approximately 30% confluence and left overnight to adhere. The following day cells are treated with Torkinib (PP 242) (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM), Rapamycin, or vehicle (0.1% DMSO). After 72 h of treatment, 10 μL of 440 μM resazurin sodium salt is added to each well, and after 18 h, 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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[2]

Mice^[2]
Six-wk-old male C57BL/6 mice are fasted overnight prior to drug treatment. Torkinib (PP 242) (0.4 mg), Rapamycin (0.1 mg), or vehicle alone is injected IP. After 30 min for the Rapamycin-treated mouse or 10 min for the Torkinib (PP 242) and vehicle-treated mice, 250 mU of insulin in 100 μL of saline is injected IP. 15 min after the insulin injection, the mice are killed by CO₂ asphyxiation followed by cervical dislocation. Tissues are harvested and frozen on liquid nitrogen in 200 μL of cap lysis buffer. The frozen tissue is thawed on ice, manually disrupted with a mortar and pestle, and then further processed with a micro tissue-homogenizer. Protein concentration of the cleared lysate is measured by Bradford assay and 5-10 μg of protein is analyzed by Western blot^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2432 mL	16.2159 mL	32.4317 mL	81.0793 mL
	5 mM	0.6486 mL	3.2432 mL	6.4863 mL	16.2159 mL
	10 mM	0.3243 mL	1.6216 mL	3.2432 mL	8.1079 mL
	15 mM	0.2162 mL	1.0811 mL	2.1621 mL	5.4053 mL
	20 mM	0.1622 mL	0.8108 mL	1.6216 mL	4.0540 mL
	25 mM	0.1297 mL	0.6486 mL	1.2973 mL	3.2432 mL
	30 mM	0.1081 mL	0.5405 mL	1.0811 mL	2.7026 mL
	40 mM	0.0811 mL	0.4054 mL	0.8108 mL	2.0270 mL
	50 mM	0.0649 mL	0.3243 mL	0.6486 mL	1.6216 mL
	60 mM	0.0541 mL	0.2703 mL	0.5405 mL	1.3513 mL
	80 mM	0.0405 mL	0.2027 mL	0.4054 mL	1.0135 mL
	100 mM	0.0324 mL	0.1622 mL	0.3243 mL	0.8108 mL

Keywords

Torkinib

30 Cited Publications

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Torkinib

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High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

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PI3K/Akt/mTOR Compound Library

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Autophagy Compound Library

Anti-Aging Compound Library

Publications Citing Use of MedChemExpress (MCE) Torkinib

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (30)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Torkinib Related Classifications

HY-10474 Related Classifications