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Chemical Structure : 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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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.
| M.Wt | 491.47 | |
| Formula | C26H20F3N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. James M Smith, et al. J Med Chem. 2024 Jul 30. doi: 10.1021/acs.jmedchem.4c00097.
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