MA242

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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 Chemical Structure

CAS No. : 1049704-18-8

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Other Forms of MA242:

MA242 free base Get quote

1 Publications Citing Use of MCE MA242

•Biochem Pharmacol. 2020 Apr;174:113795. [Abstract]

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Description

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.

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.

1049704-18-8

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Wang W, et al. Discovery and Characterization of Dual Inhibitors of MDM2 and NFAT1 for Pancreatic Cancer Therapy. Cancer Res. 2018 Oct 1;78(19):5656-5667. [Content Brief]

[2]. Wei Wang, et al. MDM2-NFAT1 dual inhibitor, MA242: Effective against hepatocellular carcinoma, independent of p53. Cancer Lett. 2019 Sep 10;459:156-167. [Content Brief]

MA242 Related Classifications

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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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