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Chemical Structure| 955977-50-1 Chemical Structure| 955977-50-1

Structure of PI-3065
CAS No.: 955977-50-1

Chemical Structure| 955977-50-1

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PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, > 70-fold selectivity over other PI3K family members.

Synonyms: PI-3065

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Product Details of PI-3065

CAS No. :955977-50-1
Formula : C27H31FN6OS
M.W : 506.64
SMILES Code : FC1=C(C2=NC(N3CCOCC3)=C4C(C=C(CN5CCN(CC6CC6)CC5)S4)=N2)C7=C(NC=C7)C=C1
Synonyms :
PI-3065
MDL No. :MFCD28167771
InChI Key :YDNOHCOYQVZOMC-UHFFFAOYSA-N
Pubchem ID :24937012

Safety of PI-3065

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

Related Pathways of PI-3065

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110β

    p110β, IC50:1078 nM

  • p110δ

    p110δ, IC50:15 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Neutrophil-like HL60 cells 150 nM 60 min To evaluate the inhibitory effect of PI3K p110δ inhibitor PI 3065 on 1,3-dithiane-induced neutrophil ROS production, results showed PI 3065 was the most potent inhibitor. Molecules. 2019 May 10;24(9):1809.
CD8+ T cells 10 µM 5 days To evaluate the effect of PI-3065 on TCF1 expression in CD8+ T cells. Results showed that PI-3065 treatment helped maintain TCF1 expression, suggesting it may promote T cell self-renewal capacity. J Immunother Cancer. 2020 Oct;8(2):e000693.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice 4T1 mammary tumor model Oral gavage 75 mg/kg Daily dosing, starting either one day before tumor inoculation or on day 7 after tumor inoculation, until the end of the experiment To evaluate the effect of PI-3065 on 4T1 mammary tumor growth. Results showed that PI-3065 significantly reduced tumor growth rate, with some mice showing tumor regression (regressors) and others showing slowed but continued tumor growth (non-regressors). Additionally, PI-3065 treatment significantly reduced the number of tumor-infiltrating regulatory T cells (Treg) and enhanced CD8+ T cell-mediated antitumor immune responses. J Immunother Cancer. 2020 Oct;8(2):e000693.
BALB/c mice 4T1 breast cancer model Oral gavage 75 mg/kg Daily dosing starting from one day before tumor injection until the end of the experiment To investigate the effect of PI3Kδ inhibition on MDSCs, results showed that PI-3065 treatment significantly reduced MDSC expansion and tumor size Br J Cancer. 2022 Nov;127(9):1595-1602
Mice Carotid artery injury model Oral gavage 75 mg/kg Once daily, starting 2 days before injury until 30 days after injury To evaluate the effect of PI-3065 on inflammatory response and restenosis after carotid injury, results showed that PI-3065 almost completely prevented restenosis after artery injury. Biosci Rep. 2017 Sep 27;37(5):BSR20171112

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL

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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