Cat. No.: HY-100026

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PQR620

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.

For research use only. We do not sell to patients.

Purity: 98.01%
CAS No.: 1927857-56-4
Formula: C₂₁H₂₅F₂N₇O₂
Molecular Weight:445.47

Storage:

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

PQR620 Chemical Structure

CAS No.: 1927857-56-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2^[1].

IC₅₀ & Target^[1]

mTORC1

mTORC2

All mTOR Isoforms :

In Vitro

PQR620 is a potent and selective mTOR inhibitor, which induces >1000-fold selectivity towards mTOR over PI3Kα in enzymatic binding assays. In A2058 melanoma cells PQR620 demonstrates inhibition of protein kinase B (pSer473) and ribosomal protein S6 (pSer235/236) phosphorylation with IC₅₀ values of 0.2 μM and 0.1 μM, respectively. PQR620 shows excellent selectivity over a wide panel of kinases, as well as excellent selectivity versus unrelated receptor enzymes and ion channels. PQR620 demonstrates its potency to prevent cancer cell growth in an NTRC 44 cancer cell line panel, resulting in a ¹⁰log(IC₅₀) of 2.86 (nM)^[1]. PQR620 has a median IC₅₀ of 250 nM when tested on 44 lymphoma cell lines. Activity is higher in B cell than in T cell tumors (median IC₅₀s: 250 nM vs 450 nM; P=0.002). At 72h, anti-tumor activityof PQR620 is mostly cytostatic and apoptosis induction is seen only in 6/44 cell lines (13%). Sensitivity to PQR620 or apoptosis induction does not differ between DLBCL and MCL, and they are not affected by the DLBCL cell of origin, by TP53 status or by the presence of MYC or BCL2 translocations^[2].

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

In Vivo

The physico-chemical properties of PQR620 result in good oral bioavailability and excellent brain penetration^[1]. The activity of PQR620 as single agent undergoes in vivo evaluation in two DLBCL models, the germinal center B cell type DLBCL (GCB-DLBCL) SU-DHL-6 and the acivated B cell-like DLBCL (ABC-DLBCL) RIVA. Treatments with PQR620 (100 mg/kg dose per day, Qd×7/w) start with 100-150 mm³ tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA). In both models, PQR620 determines a 2-fold decrease of the tumor volumes in comparison with control, with significant differences in both SU-DHL-6 (D7, D9, D11, D14; P<0.005) and RIVA (D14, D16, D19, D21; P<0.005)^[2].

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

Chemical Information

CAS No. 1927857-56-4
Appearance Solid
Molecular Weight 445.47
Formula C₂₁H₂₅F₂N₇O₂
Color White to yellow
SMILES

[H][C@]1(CC[C@]([H])2COC1)N2C3=NC(N4[C@]5([H])CC[C@]([H])4COC5)=NC(C6=CN=C(N)C=C6C(F)F)=N3
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (4)

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Journal Impact Factor

Small

High Throughput Confined Migration Microfluidic Device for Drug Screening. [Abstract]

2023 Apr;19(16):e2207194. PMID: 36634971
Int J Mol Sci

The OTX2 Gene Induces Tumor Growth and Triggers Leptomeningeal Metastasis by Regulating the mTORC2 Signaling Pathway in Group 3 Medulloblastomas. [Abstract]

2024 Apr 17;25(8):4416. PMID: 38674001
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
Front Oncol

The Anti-Non-Small Cell Lung Cancer Cell Activity by a mTOR Kinase Inhibitor PQR620. [Abstract]

2021 Jun 10:11:669518. PMID: 34178653

Solvent & Solubility

In Vitro:

DMSO : 6.4 mg/mL (14.37 mM; Need warming; 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

2.2448 mL

11.2241 mL

22.4482 mL

5 mM

0.4490 mL

2.2448 mL

4.4896 mL

10 mM

0.2245 mL

1.1224 mL

2.2448 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Protocol

Cell Assay^[2]

The drug concentration causing 50% inhibition of cell proliferation (IC₅₀) is obtained in lymphoma cell lines [diffuse large B cell lymphoma (DLBCL); mantle cell lymphoma (MCL); anaplastic large T-cell lymphoma; and others] exposed to increasing doses of PQR620 for 72 h using a Tecan D300e Digital Dispenser on 384 well plates^[2].

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

Animal Administration^[2]

Mice^[2]
For in vivo experiments, NOD-Scid (NOD.CB17-Prkdcscid/J) mice are subcutaneously inoculated with 10×10⁶ (RIVA) or with 5×10⁶(SU-DHL-6) cells. Treatments with PQR620 (100mg/kg dose per day, Qdx7/w) started with 100-150 mm³ tumors and are carried for 14 (SU-DHL-6) or 21 days (RIVA).

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

References

[1]. Florent Beaufils, et al. Abstract 1336: Structure-activity relationship studies, synthesis, and biological evaluation of PQR620, a highly potent and selective mTORC1/2 inhibitor. Cancer Research; 2016 Apr 16-20.

[2]. Chiara Tarantelli, et al. Targeting the PI3K/mTOR Pathway in Lymphoma with PQR309 and PQR620: Single Agent Activity and Synergism with the BCL2 Inhibitor Venetoclax. Blood 2016 128:3017.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2448 mL	11.2241 mL	22.4482 mL	56.1205 mL
	5 mM	0.4490 mL	2.2448 mL	4.4896 mL	11.2241 mL
	10 mM	0.2245 mL	1.1224 mL	2.2448 mL	5.6121 mL

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PQR620

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Lipid Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Mitochondrial Protection Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) PQR620

All mTOR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PQR620 Related Classifications

HY-100026 Related Classifications