Home PI3K/Akt/mTOR PI3K inhibitor PIK-294

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PIK-294 PI3K inhibitor

Cat.No.S2227

PIK-294 is a highly selective p110δ inhibitor with IC50 of 10 nM, 1000-, 49- and 16-fold less potent to PI3Kα/β/γ, respectively.
PIK-294 PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 489.53

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Quality Control

Batch: S222701 DMSO]98 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
99.9

Solubility

In vitro
Batch:

DMSO : 98 mg/mL (200.19 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Chemical Information, Storage & Stability

Molecular Weight 489.53 Formula

C28H23N7O2

 Storage (From the date of receipt)
CAS No. 900185-02-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C2C(=CC=C1)N=C(N(C2=O)C3=CC=CC=C3C)CN4C5=NC=NC(=C5C(=N4)C6=CC(=CC=C6)O)N

Mechanism of Action

Features
A p110δ inhibitor.
Targets/IC50/Ki
p110δ
(Cell-free assay)
10 nM
p110γ
(Cell-free assay)
160 nM
p110β
(Cell-free assay)
490 nM
In vitro
PIK-294 shows distinct patterns of isoform selectivity to inhibit different subsets of class I PI3K isoforms (p110β, p110δ, and p110γ) and exhibits low sensitivity to p110α with IC50 of 10 μM). The m-phenol moiety of this compound is able to penetrate the deep-affinity pocket of the ATP binding site, and thus increases in vitro inhibitory activity.
References

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