2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. EGFR PI3K PPAR
  4. MTX-531

MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors.

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MTX-531 Chemical Structure

MTX-531 Chemical Structure

CAS No. : 2791417-66-6

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Based on 1 publication(s) in Google Scholar

MTX-531 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All PI3K Isoform Specific Products:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All PPAR Isoform Specific Products:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MTX-531 is an oral drug that inhibits EGFR (with an IC50 of 14.7 nM) and PI3K (with IC50 values of 6.4, 233, 8.3, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ respectively), and it has anti-tumor effects. MTX-531 also acts as a weak agonist of PPARγ, with an IC50 of 2.5 µM, helping to alleviate hyperglycemia induced by PI3K inhibitors[1].

IC50 & Target

PI3Kα

6.4 nM (IC50)

PI3Kβ

233 nM (IC50)

PI3Kδ

1.1 nM (IC50)

PI3Kγ

8.3 nM (IC50)

PPARγ

3.4 μM (EC50)

In Vitro

MTX-531 (0-10000 nM, 2 h) shows a concentration-dependent inhibitory effect on EGFR, P13K, and mTOR in CAL-33 cells[1].
MTX-531 is 3.4 μM with EC50 in 293H cells[1].
MTX-531 (10 μM, 8-24 h) activates PPARγ in 3T3-L1 cells[1].

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

MTX-531 Related Antibodies

Western Blot Analysis[1]

Cell Line: CAL-33
Concentration: 0, 10, 30, 100, 300, 1000, 3000, 10000 nM
Incubation Time: 2 h
Result: Suppressed EGFR, P13K, and mTOR in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: 3T3-L1
Concentration: 10 μM
Incubation Time: 8 and 24 h
Result: Increased expression levels of PPARγ1 and PPARγ2.
In Vivo

MTX-531 (100 mg/kg, orally, single dose) inhibits EGFR and PI3K-mTOR pathway signaling in a time-dependent manner in mice[1].
MTX-531 (25 mg/kg, orally, once daily for 134-145 days) suppresses tumor proliferation in mice[1].
MTX-531 (100 mg/kg, orally, single dose) shows excellent tolerance in mice and uniquely does not cause the hyperglycemia commonly seen with PI3K inhibitors[1].
MTX-531 (100 mg/kg, orally, single dose) inhibits EGFR and PI3K-mTOR signaling and tumor growth in the HNSCC PDX model[1].
MTX-531 enhances MEK inhibition in CRC[1].
MTX-531 (100 mg/kg, orally, 0-35 days) combined with KRAS-G12C inhibitors suppresses tumor growth in mice with KRAS-G12C mutant colorectal cancer or pancreatic tumors[1].

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

Animal Model: CAL-33 tumor-bearing mice[1]
Dosage: 100 mg/kg; single dose
Administration: Oral
Result: Inhibited the EGFR and PI3K-mTOR signaling pathways with time-dependent.
Animal Model: CAL-33 tumor-bearing mice; CAL-27 tumor-bearing mice[1]
Dosage: 25mg/kg; daily; 134 days for CAL-33; 145 days for CAL-27
Administration: Oral
Result: Was very effective against CAL-33 and CAL-27 xenografts, showing a complete remission rate of 33-100% over a broad dosage range, and worked well for advanced CAL-33 tumors before treatment.
Molecular Weight

453.94

Formula

C22H20ClN5O2S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

ClC1=C(NS(=O)(C)=O)C=C(C2=CC3=C(N=CN=C3N[C@@H](C4=CC=CC=C4)C)C=C2)C=N1
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 (220.29 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 2.2029 mL 11.0147 mL 22.0293 mL
5 mM 0.4406 mL 2.2029 mL 4.4059 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
=
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: ≥ 5 mg/mL (11.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 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 2.2029 mL 11.0147 mL 22.0293 mL 55.0734 mL
5 mM 0.4406 mL 2.2029 mL 4.4059 mL 11.0147 mL
10 mM 0.2203 mL 1.1015 mL 2.2029 mL 5.5073 mL
15 mM 0.1469 mL 0.7343 mL 1.4686 mL 3.6716 mL
20 mM 0.1101 mL 0.5507 mL 1.1015 mL 2.7537 mL
25 mM 0.0881 mL 0.4406 mL 0.8812 mL 2.2029 mL
30 mM 0.0734 mL 0.3672 mL 0.7343 mL 1.8358 mL
40 mM 0.0551 mL 0.2754 mL 0.5507 mL 1.3768 mL
50 mM 0.0441 mL 0.2203 mL 0.4406 mL 1.1015 mL
60 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9179 mL
80 mM 0.0275 mL 0.1377 mL 0.2754 mL 0.6884 mL
100 mM 0.0220 mL 0.1101 mL 0.2203 mL 0.5507 mL
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MTX-531 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:

MTX-5312791417-66-6MTX531MTX 531EGFRPI3KPPAREpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasePeroxisome proliferator-activated receptorssquamous head and neck patient-derived xenograft (PDX) modelsCRCInhibitorinhibitorinhibit

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