Chemical Structure : AZ-PRMT5i-1
CAS No.:
2918814-96-5
AZ-PRMT5i-1
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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491.47
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Formula
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C26H20F3N5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. James M Smith, et al. J Med Chem. 2024 Jul 30. doi: 10.1021/acs.jmedchem.4c00097.
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