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MA242

MA242

Catalog No.: PC0062

Size: 50 mg, 100mg, 250mg.


Description

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

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
Shipping Room temperature in continental US; may vary elsewhere.
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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.
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.
MA242 decreases cell proliferation and induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
MA242 alone or in combination with Gemcitabine inhibits pancreatic tumor growth and metastasis without any host toxicity.
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.
In Vivo MA242 (IP; 2.5, 5, 10 mg/kg) suppresses orthotopic pancreatic tumor growth in vivo, independent of p53.
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.
All of our services are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.