2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. MA242

MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status.

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MA242

MA242 Chemical Structure

CAS No. : 1049704-18-8

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Based on 1 publication(s) in Google Scholar

Other Forms of MA242:

MA242 Related Antibodies

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Description

MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].

IC50 & Target

MDM2, NFAT1[1]
In Vitro

MA242 (0.05-5 μM; 72 hours) significantly inhibits pancreatic cancer cell growth, with IC50s ranging from 0.1 to 0.4 μM, regardless of the p53 status of the cells. However, MA242 shows minimal effects on the growth of normal HPDE cells (IC50=5.81 μM), indicating that MA242 has selective effects against cancer cells[1].
MA242 (0.1-0.5 μM; 24 hours) significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1].
MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1].
MA242 exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 shows selective cytotoxicity against HCC cells, with IC50 values ranging from 0.1-0.31 μM[2].

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

MA242 Related Antibodies

Cell Viability Assay[1]

Cell Line: The human pancreatic cancer HPAC, Panc-1, AsPC-1, Mia-Paca-2 and BxPC-3 cell lines; The human pancreatic ductal epithelium (HPDE) cell line
Concentration: 0.05, 0.5, and 5 μM
Incubation Time: 72 hours
Result: The IC50s are 0.14, 0.14, 0.15, 0.25, 0.40, and 5.81 μM for Panc-1, Mia-Paca-2, AsPC-1, BxPC-3, HPAC, and HPDE cells, respectively.

Western Blot Analysis[1]

Cell Line: The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines
Concentration: 0, 0.1, 0.2, and 0.5 μM
Incubation Time: 24 hours
Result: Decreased the expression of MDM2 and NFAT1.
In Vivo

MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53[1].
There were no significant differences in the average body weights between the vehicle- and MA242-treated mice in either of the models, did not have significant host toxicity at these effective doses[1].

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

Animal Model: Female 4-6-week-old athymic nude mice (nu/nu, 4-6 weeks) bearing AsPC-1-Luc or Panc-1-Luc tumor[1]
Dosage: 2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
Administration: IP; 2.5 or 5 mg/kg/d, 5 d/wk for five weeks for Panc-1 tumor-bearing mice;
IP; 10 mg/kg/d, 5 d/wk for three weeks for AsPC-1 tumor-bearing mice
Result: Resulted in 56.1% and 82.5% inhibition of tumor growth in nude mice bearing Panc-1 orthotopic tumors, respectively.
Significantly suppressed the growth of AsPC-1 orthotopic tumors by 89.5% (P < 0.01) compared with the tumors in control animals.
Led to almost complete tumor regression in MD242-treated mice in both models.
Molecular Weight

579.98

Formula

C26H21ClF3N3O5S
CAS No.
Appearance

Solid

Color

Purple to dark purple

SMILES

O=C1C(NCC2=CC=C(Cl)C=C2)=CC3=NCCC4=CN(S(=O)(C5=CC=C(C)C=C5)=O)C1=C34.FC(F)(C(O)=O)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (86.21 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 1.7242 mL 8.6210 mL 17.2420 mL
5 mM 0.3448 mL 1.7242 mL 3.4484 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (4.31 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.31 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 1.7242 mL 8.6210 mL 17.2420 mL 43.1049 mL
5 mM 0.3448 mL 1.7242 mL 3.4484 mL 8.6210 mL
10 mM 0.1724 mL 0.8621 mL 1.7242 mL 4.3105 mL
15 mM 0.1149 mL 0.5747 mL 1.1495 mL 2.8737 mL
20 mM 0.0862 mL 0.4310 mL 0.8621 mL 2.1552 mL
25 mM 0.0690 mL 0.3448 mL 0.6897 mL 1.7242 mL
30 mM 0.0575 mL 0.2874 mL 0.5747 mL 1.4368 mL
40 mM 0.0431 mL 0.2155 mL 0.4310 mL 1.0776 mL
50 mM 0.0345 mL 0.1724 mL 0.3448 mL 0.8621 mL
60 mM 0.0287 mL 0.1437 mL 0.2874 mL 0.7184 mL
80 mM 0.0216 mL 0.1078 mL 0.2155 mL 0.5388 mL
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MA242 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:

MA2421049704-18-8MA 242MA-242MDM-2/p53ApoptosisMDM2NFAT1p53-independentCRISPR/Cas9Pancreatic CancerHepatocellular carcinomapatient-derived xenograftInhibitorinhibitorinhibit

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