Anvumetostat (AMG 193) | PRMT5 inhibitor

Chemical Structure : AMG 193

CAS No.: 2790567-82-5

AMG 193 (Anvumetostat, AMG-193, AMG193)

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

Anvumetostat (AMG 193, 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).

Packing	Price	Stock
5 mg	$58	In stock
10 mg	$88	In stock
25 mg	$138	In stock
50 mg	$218	In stock
100 mg		Get quote

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Biological Activity

Anvumetostat (AMG 193, 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.

AMG 193 (Anvumetostat, AMG-193, AMG193)

Biological Activity

Physicochemical Properties

References

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