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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-AM-9747
AM-9747

Chemical Structure : AM-9747

CAS No.: 2691869-82-4

AM-9747 (AM9747)

货号: PC-22809Not For Human Use, Lab Use Only.

AM-9747 (AM9747) is a potent, selective and MTA cooperative PRMT5 inhibitor, inhibits symmetrical dimethyl arginine methylation (SDMA) levels in HCT116 MTAP-deleted cells with IC50 of 2 nM.

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

生物&药学活性

AM-9747 (AM9747) is a potent, selective and MTA cooperative PRMT5 inhibitor, inhibits symmetrical dimethyl arginine methylation (SDMA) levels in HCT116 MTAP-deleted cells with IC50 of 2 nM.
AM-9747 selectively inhibited the proliferation of HCT116 MTAP-deleted cells (IC50 = 0.027 μM) compared to HCT116 MTAP-WT cells (IC50 = 0.63 μM).
AM-9747 inhibited the proliferation of most MTAP-deleted cells, with minimal effects on MTAP-WT cells.
AM-9747 induces DNA damage, as illustrated by increased phosphorylation of H2AX, and an arrest in the G2/M phase of the cell cycle in MTAP-deleted cells.
AM-9747 selectively inhibits SDMA and tumor growth in HCT116 MTAP-deleted tumor xenografts, compared to HCT116 MTAP-WT xenografts.

物理化学性质&存储条件

分子量 466.47
分子式 C24H21F3N6O
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

(R)-2-amino-3-methyl-N-(1-(pyrimidin-2-yl)ethyl)-N-((5-(trifluoromethyl)pyridin-2-yl)methyl)quinoline-6-carboxamide

参考文献

1. Brian Belmontes, et al. Cancer Res (2022) 82 (12_Supplement): 1807.

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