ChemicalBook >> CAS DataBase List >>Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]-

Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]-

Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- structure

CAS No.: 1049704-17-7

Chemical Name:: Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]-

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]-

CBNumber:: CB510906953

Molecular Formula:: C24H20ClN3O3S

Molecular Weight:: 465.95

MDL Number:

MOL File:: 1049704-17-7.mol

MSDS File:: SDS

Last updated:2025-04-18 09:52:22

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Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- Properties

Boiling point	687.3±65.0 °C(Predicted)
Density	1.44±0.1 g/cm3(Predicted)
pka	2.52±0.20(Predicted)

Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- Chemical Properties,Uses,Production

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.

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

Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- Preparation Products And Raw materials

Raw materials

Preparation Products

Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- Suppliers

Global( 2)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
BOC Sciences	1-631-485-4226; 16314854226	info@bocsci.com	United States	9920	65
TargetMol Chemicals Inc.	15002134094	marketing@targetmol.cn	China	29874	58

Supplier	Advantage
BOC Sciences	65
TargetMol Chemicals Inc.	58

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Pyrrolo[4,3,2-de]quinolin-8(1H)-one, 7-[[(4-chlorophenyl)methyl]amino]-3,4-dihydro-1-[(4-methylphenyl)sulfonyl]- MA242 free base 1049704-17-7