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PI-3065 PI3K inhibitor

Cat.No.S7623

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

Chemical Structure

Molecular Weight: 506.64

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Chemical Information, Storage & Stability

Molecular Weight 506.64 Formula

C27H31FN6OS

 Storage (From the date of receipt)
CAS No. 955977-50-1 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CC1CN2CCN(CC2)CC3=CC4=C(S3)C(=NC(=N4)C5=C(C=CC6=C5C=CN6)F)N7CCOCC7

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (197.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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%
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
p110δ [1]
(Cell-free assay)
15 nM
p110β [1]
(Cell-free assay)
1078 nM
In vitro
PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ. [1]
In vivo
In mouse model, PI-3065 (75 mg/kg, p.o.) also suppresses 4T1 tumor growth and metastasis via inactivation of p110δ. In the LSL.KrasG12D/+; p53R172H/+; PdxCretg/+ (or KPC) model of pancreatic ductal adenocarcinoma, this compound prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies. [1]
References

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