PQR620

Catalog No.S8784 Batch:S878401

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Technical Data

Formula

C21H25F2N7O2
Molecular Weight 445.47 CAS No. 1927857-56-4
Solubility (25°C)* In vitro DMSO 20 mg/mL (44.89 mM)
Ethanol 2 mg/mL (4.48 mM)
Water ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Cell Assay:

[1]
  • 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.
Animal Study:

[1]
  • Animal Models

    NOD-Scid mice with RI-1/SU-DHL-6 xenograft

  • Dosages

    50 mg/kg, 100 mg/kg

  • Administration

    Oral gavage

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.