Bimiralisib (PQR309)

For research use only.

Catalog No.S8738

1 publication

Bimiralisib (PQR309) Chemical Structure

Molecular Weight(MW): 411.38

Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.

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Selleck's Bimiralisib (PQR309) has been cited by 1 publication

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Biological Activity

Description Bimiralisib (PQR309) is a novel brain-penetrant dual PI3K/mTOR inhibitor with in vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3K-related lipid kinases, protein kinases and unrelated targets.
Targets
PI3Kα [2]
(Cell-free assay)
PI3Kβ [2]
(Cell-free assay)
mTOR [2]
(Cell-free assay)
PI3Kγ [2]
(Cell-free assay)
PI3Kδ [2]
(Cell-free assay)
1.5 nM(Kd) 11 nM(Kd) 12 nM(Kd) 25 nM(Kd) 25 nM(Kd)
In vitro

PQR309 shows in vitro activity with a median IC50 value of 233 nmol/L (95% CI, 174-324 nmol/L) in most of the tesed lymphoma cell lines (increasing doses, 72 hours). The arrest in proliferation is mainly due to cell cycle arrest with a block in G1 rather than to apoptosis, limited to only 2/7 cell lines. PQR309 is more active in B-cell lymphoma cell lines (DLBCL, MCL, CLL, and SMZL) than in the T-cell derived ALCL. PQR309 inhibits PI3K/mTOR signaling in lymphoma cell lines. It has in vitro and in vivo antilymphoma activity as single agent and in combination[1]

In vivo

PQR309 is orally available, crosses the blood−brain barrier, and displayed favorable pharmacokinetic parameters in mice, rats, and dogs. It shows little clearance when exposed to rat, dog, and human liver microsomes, with a quicker turnover of PQR309 in mouse liver microsomes, where 40% of the compound was eliminated within 30 min. In female mice, plasma concentrations of PQR309 depended on the drug administration route, resulting in half-lives of approximately 13-36 min for po administration vs 9-10 min for iv administration. PQR309 shows excellent oral bioavailability (>50%). Male Beagle dogs, exposed to PQR309 at 10 mg/kg po, showed maximal drug plasma concentrations Cmax of 583 ng/mL (approximately 1.5 μM) after 60-90 min and a half-life of >7 h, which results in drug levels of approximately 0.38 μM (150 ng/mL) after 24 h. The oral bioavailability in male Beagle dogs was estimated to be 23%. Altogether the PK studies in the three models (female CD-1 mouse, female Sprague-Dawley rats, male Beagle dog) show rapid absorption of PQR309 and good oral bioavailability. PQR309 demonstrates efficiency in inhibiting proliferation in tumor cell lines (PC3 prostate cancer cells) and a rat xenograft model (PC3 xenograft model)[2].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: lymphoma cell lines
  • Concentrations: 500 nmol/L
  • Incubation Time: 72 h
  • Method:

    --


    (Only for Reference)
Animal Research:

[2]

- Collapse
  • Animal Models: female CD-1 mice, female Sprague-Dawley rats, and male Beagle dogs
  • Dosages: 5 mg/kg (i.v) or 10 mg/kg (oral)
  • Administration: by either a single intravenous bolus or a single oral application
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 6 mg/mL (14.58 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 411.38
Formula

C17H20F3N7O2

CAS No. 1225037-39-7
Storage powder
in solvent
Synonyms N/A
Smiles C1COCCN1C2=NC(=NC(=N2)C3=CN=C(C=C3C(F)(F)F)N)N4CCOCC4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02483858 Completed Drug: PQR 309 Cancer PIQUR Therapeutics AG|Roswell Park Cancer Institute|M.D. Anderson Cancer Center|Mayo Clinic|Hospital Clinic of Barcelona|University College London Hospitals|Churchill Hospital|Case Western Reserve University|University Hospital Zürich March 21 2019 Phase 1
NCT03127020 Completed Drug: PQR309 Lymphoma|Non-Hodgkin Lymphoma PIQUR Therapeutics AG|University Hospital Basel Switzerland|University Hospital Munich|University Hospital Freiburg|Charite University Berlin Germany|University of Stuttgart June 2016 Phase 2
NCT02723877 Completed Drug: PQR309|Drug: Eribulin Metastatic Breast Cancer PIQUR Therapeutics AG|Hospital Universitario Ramon y Cajal|Hospital Universitari Vall d''Hebron Research Institute|Institut Català d''Oncologia|Churchill Hospital|Barts Cancer Institute|Fundación Instituto Valenciano de Oncología March 28 2016 Phase 1|Phase 2
NCT02850744 Terminated Drug: PQR309 Glioblastoma Multiforme PIQUR Therapeutics AG|University Hospital Basel Switzerland|University Hospital Inselspital Berne|University Hospital Zürich July 2015 Phase 2
NCT02249429 Completed Drug: bimiralisib Lymphoma Malignant PIQUR Therapeutics AG|University College London Hospitals|Churchill Hospital|Royal Marsden NHS Foundation Trust|University of Haifa|Weill Medical College of Cornell University|Institut Curie|University Clinical Center Sarajevo|Clinical Center Kragujevac|Clinical Center Nis Nis|Institute for Oncology and Radiology Serbia Belgrade|University Clinical Center Republic of Srpska Banja Luka May 2015 Phase 2

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID