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Chemical Structure| 1225037-39-7 Chemical Structure| 1225037-39-7

Structure of Bimiralisib
CAS No.: 1225037-39-7

Chemical Structure| 1225037-39-7

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PQR309 is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively.

Synonyms: PQR309; PI3K-IN-2

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Product Details of Bimiralisib

CAS No. :1225037-39-7
Formula : C17H20F3N7O2
M.W : 411.38
SMILES Code : NC1=NC=C(C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2)C(C(F)(F)F)=C1
Synonyms :
PQR309; PI3K-IN-2
MDL No. :MFCD28902193
InChI Key :ADGGYDAFIHSYFI-UHFFFAOYSA-N
Pubchem ID :58507717

Safety of Bimiralisib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Bimiralisib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, Kd:25 nM

  • p110β

    PI3Kβ, Kd:11 nM

  • p110α

    PI3Kα, Kd:1.5 nM

  • p110δ

    PI3Kδ, Kd:25 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HEC-1A cells 0, 0.25, 0.5, 1, 2 μM 72 hours To evaluate the effect of PQR309 on the survival of endometrial cancer cells, results showed that PQR309 inhibited cell viability in a dose-dependent manner. PMC8616154
Ishikawa cells 0, 0.25, 0.5, 1, 2 μM 72 hours To evaluate the effect of PQR309 on the survival of endometrial cancer cells, results showed that PQR309 inhibited cell viability in a dose-dependent manner. PMC8616154
HEC-59 cells 0, 0.25, 0.5, 1, 2 μM 72 hours To evaluate the effect of PQR309 on the survival of endometrial cancer cells, results showed that PQR309 inhibited cell viability in a dose-dependent manner. PMC8616154
AN3CA cells 0, 0.25, 0.5, 1, 2 μM 72 hours To evaluate the effect of PQR309 on the survival of endometrial cancer cells, results showed that PQR309 inhibited cell viability in a dose-dependent manner. PMC8616154
ML-2 1 μM 20 hours To evaluate the effects of Bimiralisib in TP53 mutated AML cells. Results showed that Bimiralisib combined with Venetoclax significantly enhanced apoptosis and cell death. PMC9604078
SKM-1 1 μM 20 hours To evaluate the effects of Bimiralisib in TP53 mutated AML cells. Results showed that Bimiralisib combined with Venetoclax significantly enhanced apoptosis and cell death. PMC9604078
MOLM-13 1 μM 20 hours To evaluate the effect of PLX51107 on AML cell viability, results showed that PLX51107 reduced AML cell viability PMC9604078
OCI-AML3 10 μM 20 hours CGM097 showed synergy with AZD6244 in OCI-AML3 cells PMC9604078
SKOV3 cells 2 μM 24 hours To evaluate the effect of PFK158 on PARPi resistance, results showed that PFK158 inhibited PFKFB3 activity and enhanced PARPi sensitivity. PMC5656176
A2058 cells 5 μM 24 hours Induced G1 cell cycle arrest PMC5656176
TMD8 1 µM 4, 8, 12 hours To study transcriptional changes after PIK3/mTOR inhibition PMC8167571
U2932 1 µM 4, 8, 12 hours Evaluate the inhibitory effect of AMD3465 on CXCR4 expression, results showed AMD3465 partially inhibited the binding of [18F]MCFB PMC8167571

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude rats PC3 xenograft model Oral 5, 10, 15 mg/kg Once daily for 28 days Significantly inhibited tumor growth in a dose-dependent manner PMC5656176

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02850744 Glioblastoma Multiforme PHASE2 TERMINATED 2025-11-17 University Hospital Zurich, Ne... More >>urology, Zurich, 8091, Switzerland Less <<
NCT01940133 Advanced Solid Tumors PHASE1 COMPLETED 2025-12-15 University Hospital Basel, Bas... More >>el, 4031, Switzerland Less <<
NCT02669511 Primary Central Nervous System... More >> Lymphoma Less << PHASE2 COMPLETED 2018-01-12 -
NCT03127020 Lymphoma|Non-Hodgkin Lymphoma PHASE2 COMPLETED - Medizinische Klinik und Polikl... More >>inik III, Munich, Bavaria, 81377, Germany Less <<
NCT03120000 Primary Central Nervous System... More >> Lymphoma Less << PHASE2 WITHDRAWN 2025-12-19 Aix-Marseilles Université, Mar... More >>seille, 13305, France|Service de Neurology CHRU de Nancy, Nancy, 54035, France|H?pital Pitié-Salpétrier,, Paris, 75013, France|Hématologie, Départment d'ongolgie médicale, Saint-Herblain, 44800, France Less <<
NCT03740100 HNSCC PHASE2 TERMINATED 2020-12-09 M.D. Anderson Cancer Center, H... More >>ouston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.15mL

2.43mL

1.22mL

24.31mL

4.86mL

2.43mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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