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AMG193

Chemical Structure : AMG193

CAS No.: 2790567-82-5

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AMG193 (AMG-193)

Catalog No.: PC-22135Not For Human Use, Lab Use Only.

AMG193 (AMG-193) is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of 107 nM in MTAP deleted cells, binds to the PRMT5-MTA complex with an extremely high affinity (3.9 pM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AMG193 (AMG-193) is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of 107 nM in MTAP deleted cells, binds to the PRMT5-MTA complex with an extremely high affinity (3.9 pM).
AMG193 induces DNA damage, cell cycle arrest, and aberrant alternative mRNA splicing in MTAP-deleted cells.
AMG193 induces robust antitumor activity and is well tolerated with no impact on normal hematopoietic cell lineages, in human cell line and patient-derived xenograft models.
AMG193 synergizes with chemotherapies or the KRAS G12C inhibitor sotorasib in vitro, and combination treatment in vivo significantly inhibits tumor growth.

Physicochemical Properties

M.Wt 444.41
Formula C22H19F3N4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(4-Amino-1,3-dihydrofuro[3,4-c][1,7]naphthyridin-8-yl)[(3S)-3-[4-(trifluoromethyl)phenyl]-4-morpholinyl]methanone

References

1. Patent WO2022132914A1.
2. Adam Radzimierski, et al. Cancer Res (2024) 84 (6_Supplement): 4598.
3. Belmontes B, et al. Cancer Discov. 2024 Sep 16. doi: 10.1158/2159-8290.CD-24-0887.

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