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MA242 free base

CAS No. : 1049704-17-7

MCE 站：MA242 free base

产品活性：MA242 free base 是特异性的 MDM2 和 NFAT1 双重抑制剂。MA242 free base 以高亲和力直接结合 MDM2 和 NFAT1，诱导 MDM2 和 NFAT1 蛋白降解，并抑制 NFAT1 介导的 MDM2 转录。MA242 free base 在胰腺癌细胞系中诱导凋亡。

研究领域：Apoptosis

作用靶点：MDM-2/p53  |  Apoptosis

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.
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.
MA242 free base decreases cell proliferation ａnd induces apoptosis in pancreatic cancer cell lines regardless of p53 status.
MA242 free base alone or in combination with Gemcitabine inhibits pancreatic tumor growth ａnd metastasis without any host toxicity.
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.

In Vivo: MA242 (IP; 2.5, 5, 10 mg/kg) free base 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 free base-treated mice in either of the models, did not have significant host toxicity at these effective doses.

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