2. PI3K/Akt/mTOR Apoptosis
  3. Akt Apoptosis
  4. PHT-427

PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 μM and 5.2 μM and for Akt and PDPK1, respectively.

For research use only. We do not sell to patients.

PHT-427 Chemical Structure

PHT-427 Chemical Structure

CAS No. : 1191951-57-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

PHT-427 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PHT-427

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 μM and 5.2 μM and for Akt and PDPK1, respectively.

IC50 & Target[1]

PDPK1

5.2 μM (Ki)

Cellular Effect
Cell Line Type Value Description References
BXPC-3 IC50
57 μM
Compound: 29
Cytotoxicity against human BxPC3 cells by MTT assay
Cytotoxicity against human BxPC3 cells by MTT assay
[PMID: 21353784]
BXPC-3 IC50
6.3 μM
Compound: 14
Inhibition of Akt phosphorylation in human BxPC3 cells by Western blotting
Inhibition of Akt phosphorylation in human BxPC3 cells by Western blotting
[PMID: 19734051]
In Vitro

The effects of PHT-427 on cell signaling are investigated by RPPA using a panel of 86 antibodies to phospho- and non-phosphorylated signaling protein related to PtdIns-3-K/PDPK1/Akt signaling in PC-3 prostate cells where PtdIns-3-K/PDPK1/Akt signaling is activated because of homozygous PTEN mutation. After 16 hours, a reduction is observed in phospho-Ser241-PDPK1 phospho-Thr308-Akt by both 10 μM PH-427 and 0.1 μM Wortmannin. Finally, phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and Wortmannin. These results suggest that at 10 μM PHT-427 inhibits both Akt and PDKP1. The BxPC-3 and MiaPaCa-2 pancreatic cancer cell lines are probed by Western blotting following up to 24 hr exposure to 10 μM PHT-427, which is below the IC50 for cell growth inhibition of around 30 μM, to determine the effects of PHT-427 on of the PtdIns-3-K/PDPK1/Akt signaling pathway components[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PHT-427 Related Antibodies
In Vivo

Mice with BxPC-3 pancreatic, MCF-7 breast or A-549 NSCL cancer xenografts are administered PHT-427, or its analogs with a C-4, C-6 or C-8 alkyl chain by oral gavage twice a day for 10 days. The results show that PHT-427 has the greatest antitumor activity with the C-8 chain analog having less activity, and analogs with a C-4 or C-6 chain very little activity. All further antitumor studies are conducted using compound PHT-427. Plasma levels of PHT-427 following oral administration to mice of a dose of 200 mg/kg show rapid absorption, without a lag phase, Cmax is 8.2 μg/mL 1 hr following dosing, and the elimination half-life is 1.4 hr with a terminal PHT-427 concentration of 0.1 μg/mL 10 hr after dosing. The plasma concentration of PH-427 is above the level which gave inhibition of Akt and PDPK1 signaling in cells of 10 μM (4 μg/mL) for at least 3 hr[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

409.61

Formula

C20H31N3O2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCCC1=CC=C(C=C1)S(NC2=NN=CS2)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (61.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4413 mL 12.2067 mL 24.4135 mL
5 mM 0.4883 mL 2.4413 mL 4.8827 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

Panc-1 cells stably transfected with green fluorescent protein (GFP) tagged Akt or PDKP1 PH domains are serum starved in phenol red free growth medium on glass-bottom 96-well imaging plates for 16 hours. They are then treated with PHT-427 at 1, 5, and 10 µM or PI-103 for 4 hr, and stimulated with 50 ng/mL IGF-1 for 10 min. Images are taken before and after IGF-1 treatment using an IN Cell Analyzer 1000 instrument with a Nikon Plan Fluor ELWD 20X/0.45 objective loaded and using a 300msec exposure time[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Female C57Bl/6 mice are administered PHT-427 as a single oral dose of 200 mg/kg. The mice are killed at different times (3 mice at each time point), blood collected into heparinized tubes and plasma prepared and stored frozen at -80°C. For assay 0.2 mL plasma is mixed with 0.2 mL of 0.1 M sodium phosphate buffer, pH 4.0, and extracted for 1 hr by inversion with 1 ml ethyl acetate. After centrifugation 0.8 mL of the organic layer is removed, evaporated under N2 and redissolved in 0.2 mL ethanol and 10 µL injected onto a Waters Quattro Ultima tandem mass spectrometer using a Phenomenex Luna 3.0 µm, 2.0×50 mm C8 analytical column with detection and quantification by multiple reaction monitoring with the mass spectrometer operating in electrospray positive ionization mode.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4413 mL 12.2067 mL 24.4135 mL 61.0337 mL
5 mM 0.4883 mL 2.4413 mL 4.8827 mL 12.2067 mL
10 mM 0.2441 mL 1.2207 mL 2.4413 mL 6.1034 mL
15 mM 0.1628 mL 0.8138 mL 1.6276 mL 4.0689 mL
20 mM 0.1221 mL 0.6103 mL 1.2207 mL 3.0517 mL
25 mM 0.0977 mL 0.4883 mL 0.9765 mL 2.4413 mL
30 mM 0.0814 mL 0.4069 mL 0.8138 mL 2.0345 mL
40 mM 0.0610 mL 0.3052 mL 0.6103 mL 1.5258 mL
50 mM 0.0488 mL 0.2441 mL 0.4883 mL 1.2207 mL
60 mM 0.0407 mL 0.2034 mL 0.4069 mL 1.0172 mL
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PHT-427 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PHT-4271191951-57-1PHT427PHT 427AktApoptosisPKBProtein kinase BInhibitorinhibitorinhibit

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