| Identification | Back Directory | [Name]
Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- | [CAS]
1049704-17-7 | [Synonyms]
MA242 free base
Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- | [Molecular Formula]
C24H20ClN3O3S | [MOL File]
1049704-17-7.mol | [Molecular Weight]
465.95 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
MA242 (IP; 2.5, 5, 10 mg/kg) free base 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 free base-treated mice in either of the models, did not have significant host toxicity at these effective doses[1]. | 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.
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| [References]
[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. DOI:10.1158/0008-5472.CAN-17-3939
[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. DOI:10.1016/j.canlet.2019.114429 |
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