Bimiralisib (PQR309)

Catalog No.S8738

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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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]

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

    --


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: female CD-1 mice, female Sprague-Dawley rats, and male Beagle dogs
  • Formulation: DMSO/20% HPBCD solution, 10/90, v/v
  • 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

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID