Home PI3K/Akt/mTOR mTOR inhibitor PQR620 For research use only.

PQR620

PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.

PQR620 Chemical Structure

PQR620 Chemical Structure

CAS No. 1927857-56-4

Purity & Quality Control

Batch: S878401 DMSO]20 mg/mL]false]Ethanol]2 mg/mL]false]Water]˂1 mg/mL]false Purity: 98.26%
98.26

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Signaling Pathway

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mTOR Signaling Pathway

Biological Activity

Description PQR620 is a novel, selective, orally bioavailable and brain penetrant dual TORC1/2 inhibitor. PQR620 has anti-tumor activity across 56 lymphoma models with a median IC50 of 250 nM after 72 h of exposure.
Targets
TORC1 [1]
(Cell-based assay)		 TORC2 [1]
(Cell-free assay)
250 nM 250 nM
In vitro
In vitro

PQR620 is a novel brain penetrant dual TORC1/2 inhibitor with anti-tumor activity across 56 lymphoma cell lines with a median IC50 value of 250 nM after 72 h of exposure.[1]
Cell Research Cell lines 56 lymphoma cell lines, ABC-DLBCL cell lines (TMD8, Ri-1), GCB-DLBCL cell lines (OCI-LY-1,SU-DHL-6, DoHH2)
Concentrations 2 μM
Incubation Time 24 h, 72 h
Method

PQR620 is dissolved in dimethyl sulphoxide (DMSO) to obtain a stock concentration of 10 mM. PQR620 is assessed in a large panel of cell lines (n = 56) derived from lymphomas. Cell lines are treated with 2 μM PQR620 for 24 h or DMSO as control.
In Vivo
In vivo

PQR620 has in vivo anti-lymphoma activity and in vivo synergism with the BCL2 inhibitor venetoclax. The combination of PQR620 and venetoclax have stronger in vivo anti-tumor activity than the single agents in a xenograft model of GCB-DLBCL.[1]
Animal Research Animal Models NOD-Scid mice with RI-1/SU-DHL-6 xenograft
Dosages 50 mg/kg, 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 445.47 Formula

C21H25F2N7O2
CAS No. 1927857-56-4 SDF --
Smiles C1CC2COCC1N2C3=NC(=NC(=N3)C4=CN=C(C=C4C(F)F)N)N5C6CCC5COC6
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 20 mg/mL ( (44.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : ˂1 mg/mL


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In vivo
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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

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.

Handling Instructions

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