PQR620

For research use only.

Catalog No.S8784

PQR620 Chemical Structure

Molecular Weight(MW): 445.47

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.

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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
TORC1/2 [1]
(Cell-based 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.[1]

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]

Protocol

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: NOD-Scid mice with RI-1/SU-DHL-6 xenograft
  • Dosages: 50 mg/kg, 100 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 20 mg/mL (44.89 mM)
Water ˂1 mg/mL
Ethanol '2 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 445.47
Formula

C21H25F2N7O2

CAS No. 1927857-56-4
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2COCC1N2C3=NC(=NC(=N3)C4=CN=C(C=C4C(F)F)N)N5C6CCC5COC6

In vivo Formulation Calculator (Clear solution)

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID