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AZ-PRMT5i-1 (Compound 28) is an effective and orally active MTAP-selective PRMT5 inhibitor. AZ-PRMT5i-1 also demonstrates MTA cooperativity and exhibits both in vitro and in vivo antitumor activities, and can be used to study MTAP-deficient cancers[1][2]. | [References]
[1] Smith JM, et al. Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity. J Med Chem. 2024 Jul 30. DOI:10.1021/acs.jmedchem.4c00097
[2] Lynch J T, et al. AZ-PRMT5i-1: A potent MTAP-selective PRMT5 inhibitor with pharmacodynamic and monotherapy anti-tumor activity in MTAP-deleted tumours[J]. Cancer Research, 2023, 83(7_Supplement): 6272-6272. |
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