PI-3065

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

PI-3065 Chemical Structure

PI-3065 Chemical Structure

CAS No. 955977-50-1

Purity & Quality Control

PI-3065 Related Products

Signaling Pathway

Biological Activity

Description PI-3065 is a selective p110δ inhibitor with IC50 of 15 nM, >70-fold selectivity over other PI3K family members.
Targets
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
15 nM 1078 nM
In vitro
In vitro PI-3065 shows no inhibition on the growth of 4T1 cells, which do not expressing detectable levels of p110δ. [1]
Cell Research Cell lines 4T1 cells
Concentrations ~10 μM
Incubation Time 48 hours
Method

Proliferation of 4T1 cells is assayed following a 4-h treatment with the indicated p110δ inhibitors, then washing and MTS staining are carried out after 48 h culture.

In Vivo
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, PI-3065 prolongs survival and reduces the incidence of macroscopic metastases and other disease-associated pathologies. [1]
Animal Research Animal Models Female WT BALB/c mice bearing 4T1 tumors
Dosages 75 mg/kg, once daily
Administration p.o.

Chemical Information & Solubility

Molecular Weight 506.64 Formula

C27H31FN6OS

CAS No. 955977-50-1 SDF Download PI-3065 SDF
Smiles C1CC1CN2CCN(CC2)CC3=CC4=C(S3)C(=NC(=N4)C5=C(C=CC6=C5C=CN6)F)N7CCOCC7
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (197.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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