2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. PHT-7.3

PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity.

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PHT-7.3 Chemical Structure

PHT-7.3 Chemical Structure

CAS No. : 1614225-93-2

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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-7.3 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PHT-7.3

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K-Ras H-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity[1].

IC50 & Target

Cnk1 PH-domain[1]
In Vivo

PHT-7.3 (200 mg/kg; i.p.; daily; for 20 days) exhibits cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft[1].

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

Animal Model: Female NOD-SCID mice (mut-KRas A549 NSCLC xenografts, mut-KRas H441 NSCLC xenografts)[1]
Dosage: 200 mg/kg
Administration: Intraperitoneal injection, daily, for 20 days
Result: Exhibited cytostatic antitumor activity in the mut-KRas(G12S) A549 xenograft and mut-KRasG12V H441 xenograft .
Molecular Weight

433.52

Formula

C24H23N3O3S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(C=CC=C2)C(CC3OCCCO3)=NN1CC4=NC(C5=CC=C(C)C=C5)=CS4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (144.17 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 2.3067 mL 11.5335 mL 23.0670 mL
5 mM 0.4613 mL 2.3067 mL 4.6134 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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: ≥ 6.25 mg/mL (14.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (14.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 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 (62.5 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

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3067 mL 11.5335 mL 23.0670 mL 57.6675 mL
5 mM 0.4613 mL 2.3067 mL 4.6134 mL 11.5335 mL
10 mM 0.2307 mL 1.1533 mL 2.3067 mL 5.7667 mL
15 mM 0.1538 mL 0.7689 mL 1.5378 mL 3.8445 mL
20 mM 0.1153 mL 0.5767 mL 1.1533 mL 2.8834 mL
25 mM 0.0923 mL 0.4613 mL 0.9227 mL 2.3067 mL
30 mM 0.0769 mL 0.3844 mL 0.7689 mL 1.9222 mL
40 mM 0.0577 mL 0.2883 mL 0.5767 mL 1.4417 mL
50 mM 0.0461 mL 0.2307 mL 0.4613 mL 1.1533 mL
60 mM 0.0384 mL 0.1922 mL 0.3844 mL 0.9611 mL
80 mM 0.0288 mL 0.1442 mL 0.2883 mL 0.7208 mL
100 mM 0.0231 mL 0.1153 mL 0.2307 mL 0.5767 mL
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PHT-7.3 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-7.31614225-93-2RasInhibitorinhibitorinhibit

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