2790567-82-5
Chemical Structure
AMG-193
- CAS No.: 2790567-82-5
- Formula:C22H19F3N4O3
- Molecular Weight:444.41
IUPAC Name: (S)-(4-amino-1,3-dihydrofuro[3,4-c][1,7]naphthyridin-8-yl)(3-(4-(trifluoromethyl)phenyl)morpholino)methanone
InChIKey: BFEBTMFPRJPBTK-LJQANCHMSA-N
SMILES: O=C(N1[C@@H](C2=CC=C(C=C2)C(F)(F)F)COCC1)C3=NC=C4N=C(N)C(COC5)=C5C4=C3
Biological Activity: AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP[1][2].
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AMG-193 | 99.71% | AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP. | ||||||||||||||||||||
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- [1]. Belmontes B, et al. Abstract B177: The discovery and preclinical characterization of AMG 193, a first-in-class MTA-cooperative PRMT5 inhibitor with broad activity against MTAP-null cancers[J]. Molecular Cancer Therapeutics, 2023, 22(12_Supplement): B177-B177.
- [2]. Belmontes B, et al. AMG 193, a Clinical Stage MTA-Cooperative PRMT5 Inhibitor, Drives Antitumor Activity Preclinically and in Patients with MTAP-Deleted Cancers[J]. Cancer Discovery, 2024: OF1-OF23. [Content Brief]
Keywords
