Home Cart Sign in  
Chemical Structure| 1225037-39-7 Chemical Structure| 1225037-39-7

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

Chemical Structure| 1225037-39-7

*Storage: {[sel_prStorage]}

*Shipping: {[sel_prShipping]}

,{[proInfo.pro_purity]}

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

4.5 *For Research Use Only !

{[proInfo.pro_purity]}
Cat. No.: {[proInfo.prAm]} Purity: {[proInfo.pro_purity]}

Change View

Size Price VIP Price

US Stock

Global Stock

In Stock
{[ item.pr_size ]} Inquiry {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate,item.pr_is_large_size_no_price, item.vip_usd) ]}

US Stock: ship in 0-1 business day
Global Stock: ship in 5-7 days

  • {[ item.pr_size ]}

In Stock

- +

Please Login or Create an Account to: See VIP prices and availability

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

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
SKOV3 cells 2 μM 24 hours Induced G1 cell cycle arrest J Med Chem. 2017 Sep 14;60(17):7524-7538.
A2058 cells 5 μM 24 hours Induced G1 cell cycle arrest J Med Chem. 2017 Sep 14;60(17):7524-7538.
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. Cells. 2021 Oct 27;10(11):2916.
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. Cells. 2021 Oct 27;10(11):2916.
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. Cells. 2021 Oct 27;10(11):2916.
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. Cells. 2021 Oct 27;10(11):2916.
U2932 1 µM 4, 8, 12 hours To study transcriptional changes after PIK3/mTOR inhibition Noncoding RNA. 2021 Apr 16;7(2):26.
TMD8 1 µM 4, 8, 12 hours To study transcriptional changes after PIK3/mTOR inhibition Noncoding RNA. 2021 Apr 16;7(2):26.
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. Int J Mol Sci. 2022 Oct 20;23(20):12587.
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. Int J Mol Sci. 2022 Oct 20;23(20):12587.
MOLM-13 1 μM 20 hours To evaluate the effects of Bimiralisib in FLT3-ITD mutated AML cells. Results showed that Bimiralisib combined with Venetoclax significantly enhanced apoptosis and cell death. Int J Mol Sci. 2022 Oct 20;23(20):12587.
OCI-AML3 10 μM 20 hours To evaluate the cytotoxicity and apoptosis-inducing effects of Bimiralisib in AML cells. Results showed that Bimiralisib treatment induced G1 cell cycle arrest and significantly enhanced Venetoclax-induced apoptosis and cell death. Int J Mol Sci. 2022 Oct 20;23(20):12587.

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 J Med Chem. 2017 Sep 14;60(17):7524-7538.

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

 

Historical Records

Categories