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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AMG193
AMG193

Chemical Structure : AMG193

CAS No.: 2790567-82-5

AMG193 (AMG-193)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 444.41
分子式 C22H19F3N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
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

参考文献

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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