MA242 free base
Based on 1 publication(s) in Google Scholar
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with high affinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
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- No. CAS: 1049704-17-7
- Fòrmula: C24H20ClN3O3S
- Peso molecular:465.95
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Publications Citing Use of MedChemExpress (MCE) MA242 free base
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Actividad biológica
Descripciòn
IC50 & Target
MDM2, NFAT1[1]
In Vitro
MA242 (0.05-5 μM; 72 hours) free base 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 free base 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) free base significantly decreases the MDM2 and NFAT1 protein levels at a low concentration in all three cell lines[1].
MA242 free base decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status[1].
MA242 free base alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity[1].
MA242 free base exerts cytotoxicity against hepatocellular carcinoma (HCC) cells by inhibiting the NFAT1-MDM2 pathway in vitro, independent of p53. MA242 showed 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.
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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
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Concentration:0.05, 0.5, and 5 μM
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Incubation Time:72 hours
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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.
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Cell Line:The human pancreatic cancer HPAC, Panc-1, and AsPC-1 cell lines
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Concentration:0, 0.1, 0.2, and 0.5 μM
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Incubation Time:24 hours
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Result:Decreased the expression of MDM2 and NFAT1.
In Vivo
There were no significant differences in the average body weights between the vehicle- and MA242 free base-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.
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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]
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Dosage:2.5 or 5 mg/kg for Panc-1 tumor-bearing mice; 10 mg/kg for AsPC-1 tumor-bearing mice
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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.
Chemical Information
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No. CAS 1049704-17-7
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Peso molecular 465.95
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Fòrmula C24H20ClN3O3S
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SMILES
O=C1C(NCC2=CC=C(C=C2)Cl)=CC3=NCCC4=CN(S(=O)(C5=CC=C(C)C=C5)=O)C1=C34
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
Curcumol enhances the sensitivity of doxorubicin in triple-negative breast cancer via regulating the miR-181b-2-3p-ABCC3 axis. [Abstract]2020 Apr:174:113795. PMID: 31926937
Pureza y Documentación
Referencias
[1]. Wei Wang, 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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MA242 free base Related Classifications
HY-112816A Related Classifications
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