2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. T-1-PMPA

T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFRWT and EGFR790m, with IC50 values of 86 nM and 561.73 nM, respectively.

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

T-1-PMPA Chemical Structure

T-1-PMPA Chemical Structure

CAS No. : 1323883-62-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 130 In-stock
Solution
10 mM * 1 mL in DMSO USD 130 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 195 In-stock
25 mg USD 390 In-stock
50 mg USD 625 In-stock
100 mg USD 1000 In-stock
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Based on 1 publication(s) in Google Scholar

T-1-PMPA Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

T-1-PMPA is a potent EGFR inhibitor with apoptotic properties. T-1-PMPA effectively inhibits EGFRWT and EGFR790m, with IC50 values of 86 nM and 561.73 nM, respectively[1].

IC50 & Target[1]

EGFRWT

86 nM (IC50)

EGFRT790M

561.73 nM (IC50)

In Vitro

T-1-PMPA (0.312-10 μM; 24 h) shows significant suppression of the proliferation of HepG2 and MCF7 malignant cell lines, with IC50 values of 3.51 μM and 4.13 μM, respectively[1]. In HepG2 cells, T-1-PMPA increases the proportion of cells in the early stage of apoptosis from 0.77 to 29.17%, the late stage of apoptosis from 0.17 to 8.81%, and the overall stage from 3.05 to 42.03%. Additionally, the percentage of necrotic cells increased to 4.05% compared to 2.21% in the control cells. The qRT-PCR analysis further supported the apoptotic effects by revealing significant increases in the levels of caspase-3 and caspase-9. T-1-PMPA controlls the levels of TNFα and IL2 by 74 and 50%[1].

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

T-1-PMPA Related Antibodies

Cell Viability Assay[1]

Cell Line: HepG2 and MCF7 malignant cell lines
Concentration: 0.312 μM, 0.625 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Showed significant suppression of the proliferation of HepG2 and MCF7 malignant cell lines.
Molecular Weight

327.34

Formula

C16H17N5O3
CAS No.
Unlabeled CAS

Appearance

Solid

Color

White to off-white

SMILES

CC1=CC=C(C=C1)NC(CN2C(C3=C(N(C2=O)C)N=CN3C)=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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (305.49 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 3.0549 mL 15.2746 mL 30.5493 mL
5 mM 0.6110 mL 3.0549 mL 6.1099 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

×
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 (7.64 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 (7.64 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

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 3.0549 mL 15.2746 mL 30.5493 mL 76.3732 mL
5 mM 0.6110 mL 3.0549 mL 6.1099 mL 15.2746 mL
10 mM 0.3055 mL 1.5275 mL 3.0549 mL 7.6373 mL
15 mM 0.2037 mL 1.0183 mL 2.0366 mL 5.0915 mL
20 mM 0.1527 mL 0.7637 mL 1.5275 mL 3.8187 mL
25 mM 0.1222 mL 0.6110 mL 1.2220 mL 3.0549 mL
30 mM 0.1018 mL 0.5092 mL 1.0183 mL 2.5458 mL
40 mM 0.0764 mL 0.3819 mL 0.7637 mL 1.9093 mL
50 mM 0.0611 mL 0.3055 mL 0.6110 mL 1.5275 mL
60 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2729 mL
80 mM 0.0382 mL 0.1909 mL 0.3819 mL 0.9547 mL
100 mM 0.0305 mL 0.1527 mL 0.3055 mL 0.7637 mL
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T-1-PMPA 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:

T-1-PMPA1323883-62-0EGFRApoptosisEpidermal growth factor receptorErbB-1HER1apoptoticanticancerEGFRWT and EGFR790mcaspase-9caspase-3Inhibitorinhibitorinhibit

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