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PHT-427

Name: PHT-427
Brand: TargetMol
SKU: T2420
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

Catalog No. T2420Cas No. 1191951-57-1

Alias PHT 427, CS-0223

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

PHT-427

🥰Excellent

Purity: 99.89%

Catalog No. T2420Alias PHT 427, CS-0223Cas No. 1191951-57-1

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

Pack Size	Price	Availability
10 mg	$39	In Stock
25 mg	$79	In Stock
50 mg	$155	In Stock
100 mg	$263	In Stock
200 mg	$452	In Stock
1 mL x 10 mM (in DMSO)	$43	In Stock

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Purity:99.89%

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	PHT-427 (CS-0223) is a dual Akt (Ki: 2.7 μM) and PDPK1 (Ki: 5.2 μM) inhibitor (high-affinity binding for the PH domains of Akt and PDPK1).
Targets&IC50	PDK1:5.2 μM(Ki), Akt:2.7 μM(Ki)
In vitro	PHT-427 had an antiproliferative effect on Panc-1 cells (IC50: 65 μM). In PC-3 prostate cancer cells, PHT-427 (10 μM) significantly decreased p-Ser241-PDPK1 and p-Thr308-Akt, indicating that PHT-427 could inhibit Akt and PDKP1. PHT-427 also inhibited the translocation of the PH domains of Akt and PDKP1 in the plasma membrane. PHT-427 induced apoptosis and inhibited AKT phosphorylation, mainly at residue Ser473 and less at residue Thr308 (IC50: 6.3 μM), with no effect on all AKT protein expression.
In vivo	PHT-427 had an antiproliferative effect on Panc-1 cells (IC50: 65 μM). In PC-3 prostate cancer cells, PHT-427 (10 μM) significantly decreased p-Ser241-PDPK1 and p-Thr308-Akt, indicating that PHT-427 could inhibit Akt and PDKP1. PHT-427 also inhibited the translocation of the PH domains of Akt and PDKP1 in the plasma membrane. PHT-427 induced apoptosis and inhibited AKT phosphorylation, mainly at residue Ser473 and less at residue Thr308 (IC50: 6.3 μM), with no effect on all AKT protein expression.
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.
Synonyms	PHT 427, CS-0223

Chemical Properties

Molecular Weight	409.61
Formula	C₂₀H₃₁N₃O₂S₂
Cas No.	1191951-57-1
Smiles	CCCCCCCCCCCCc1ccc(cc1)S(=O)(=O)Nc1nncs1
Relative Density.	1.162 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (109.86 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.88 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4413 mL	12.2067 mL	24.4135 mL	122.0673 mL
5 mM	0.4883 mL	2.4413 mL	4.8827 mL	24.4135 mL
10 mM	0.2441 mL	1.2207 mL	2.4413 mL	12.2067 mL
20 mM	0.1221 mL	0.6103 mL	1.2207 mL	6.1034 mL
50 mM	0.0488 mL	0.2441 mL	0.4883 mL	2.4413 mL
100 mM	0.0244 mL	0.1221 mL	0.2441 mL	1.2207 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc