AZ-PRMT5i-1

Chemical Structure : AZ-PRMT5i-1

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货号: PC-22808Not For Human Use, Lab Use Only.

AZ-PRMT5i-1 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of 5.5 nM in symmetrical dimethyl arginine methylation (SDMA) cellular imaging assay.

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生物&药学活性

AZ-PRMT5i-1 is a potent, selective and MTA-cooperative PRMT5 inhibitor with IC50 of 5.5 nM in symmetrical dimethyl arginine methylation (SDMA) cellular imaging assay.
AZ-PRMT5i-1 has high selectivity for PRMT5 (as well as for the C449S mutant form of PRMT5) against a panel of 37 other lysine and arginine methyltransferases.
AZ-PRMT5i-1 has IC50 of 124 nM in MTAP-null LU99 lung cancer cells.
AZ-PRMT5i-1 selectively inhibits the proliferation of MTAP-deficient cancer cell lines versus cell lines that express MTAP.
AZ-PRMT5i-1 (50 mg/kg BID oral dose) exhibits strong tumor growth inhibition in MTAP-null LU99 xenograft model.

物理化学性质&存储条件

分子量	491.47
分子式	C26H20F3N5O2
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	(S)-2-[(5-Amino-6-fluoro-1H-pyrrolo[3,2-b]pyridin-2-yl)methyl]-5-fluoro-1'-(4-fluorobenzyl)spiro[isoindoline-1,3'-pyrrolidine]-2',3-dione

参考文献

1. James M Smith, et al. J Med Chem. 2024 Jul 30. doi: 10.1021/acs.jmedchem.4c00097.

AZ-PRMT5i-1

生物&药学活性

物理化学性质&存储条件

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AZ-PRMT5i-1

生物&药学活性

物理化学性质&存储条件

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