Home PI3K/Akt/mTOR Akt inhibitor - PDPK1 inhibitor PHT-427

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PHT-427 Akt inhibitor

Cat.No.S1556

PHT-427 (CS-0223) is a dual Akt and PDPK1 inhibitor (high affinity binding for the PH domains of Akt and PDPK1) with Ki of 2.7 μM and 5.2 μM, respectively.
PHT-427 Akt inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 409.61

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Chemical Information, Storage & Stability

Molecular Weight 409.61 Formula

C20H31N3O2S2

 Storage (From the date of receipt)
CAS No. 1191951-57-1 Download SDF Storage of Stock Solutions

Synonyms CS-0223 Smiles CCCCCCCCCCCCC1=CC=C(C=C1)S(=O)(=O)NC2=NN=CS2

Solubility

In vitro
Batch:

DMSO : 82 mg/mL ( (200.19 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 60 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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
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Mechanism of Action

Targets/IC50/Ki
Akt [1]
2.7 μM(Ki)
PDPK1 [1]
5.2 μM(Ki)
In vitro
PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. This compound significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that it could inhibit both Akt and PDPK1. It also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. [1] This chemical induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. It also shows antiproliferation in Panc-1 cells with IC50 of 65 μM. [2]
Kinase Assay
Surface plasmon resonance (SPR) spectroscopy binding assays
All interaction analyses are performed with a Biacore 2000, Biacore 2000 Control Software v3.2, and BIAevaluation v4.1 analysis software. The PH domain GST-fusion proteins (Akt1, IRS1, and PDK1) are immobilized on a CM5 Sensorchip using Biacore's Amine Coupling Kit to a level of 10,000 Response units (RUs). Small molecule analytes at concentrations ranging from 0.1 to 10 × the predicted KD are injected at a high flow rate (30μL/min). DMSO concentrations in all samples and running buffer are 1% (v/v) or less.
In vivo
PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. This compound gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg. [1]
References

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