Home PI3K/Akt/mTOR mTOR inhibitor PQR620

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PQR620 mTOR inhibitor

Cat.No.S8784

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

Chemical Structure

Molecular Weight: 445.47

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 20 mg/mL (44.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : ˂1 mg/mL

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In vivo
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In vivo Formulation Calculator (Clear solution)

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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 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight 445.47 Formula

C21H25F2N7O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1927857-56-4 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CC2COCC1N2C3=NC(=NC(=N3)C4=CN=C(C=C4C(F)F)N)N5C6CCC5COC6

Mechanism of Action

Targets/IC50/Ki
TORC1
(Cell-based assay)
250 nM
TORC2
(Cell-free assay)
250 nM
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.
In vivo

This compound has in vivo anti-lymphoma activity and in vivo synergism with the BCL2 inhibitor venetoclax. The combination of this chemical and venetoclax have stronger in vivo anti-tumor activity than the single agents in a xenograft model of GCB-DLBCL.
References

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