Erythrofuranosyladenine(9-beta-D-Erythrofuranosyladenine, ETA) is a nontoxic MTAP substrate. Erythrofuranosyladenine is an effective salvage agent for methylthioadenosine phosphorylase–selective therapy of T-cell acute lymphoblastic leukemia with L-alanos
MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-dependent inhibition of SDMA in MTAP-del tumors, with less SDMA modulation observed in bone marrow[1]. [1]. Christopher R. Smith, et al. Abstract LB003: Fragment based discovery of MRTX9768, a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP CDKN2A-deleted tumors. AACR Annual Meeting 2021; April 10-15, 2021 and May 17-21, 2021; Philadelphia, PA.[2]. Yingqing Chen, et al. Targeting protein arginine methyltransferase 5 in cancers: Roles, inhibitors and mechanisms. Biomed Pharmacother. 2021 Oct 4;144:112252.
MAT2A-IN-5, a potent inhibitor of MAT2A, effectively targets the abnormally elevated expression of MAT2A found in various tumor types such as gastric, colon, liver, and pancreatic cancers. By reducing the proliferative activity of MTAP-deficient cancer cells, MAT2A-IN-5 exhibits potential in cancer research applications [1].
MAT2A-IN-7, a potent inhibitor of the enzyme MAT2A, demonstrates efficacy in targeting the abnormally elevated expression of MAT2A observed in gastric, colon, liver, and pancreatic cancers. Furthermore, MAT2A-IN-7 effectively reduces the proliferative activity specifically in MTAP-deficient cancer cells, thus highlighting its potential for cancer research applications [1].
AGI-25696 is a MATA2 inhibitor that are useful as therapeutic agents for treating malignancies. AGI-25696 showed in vivo activity in MTAP null tumors. Note: The correct structure of AGI-25696 is CAS#2201065-84-9. Many vendors mistakenly listed CAS#2201066-35-3 as its AGI25696. J. Med. Chem. 2021, 64, 8, 4430–4449 published AGI25696 structure (it is CAS#2201065-84-9).