Catalog No.: PC-22132Not For Human Use, Lab Use Only.
TNG908 (Ralometostat, TNG-908) is a potent, selective, brain penetrant, MTA-cooperative PRMT5 inhibitor with IC50 of 9 nM in SDMA in-cell western assay, binds the PRMT5·MTA complex, selectively kills MTAP-deleted (MTAP-null) cells.
TNG908 (Ralometostat, TNG-908) is a potent, selective, brain penetrant, MTA-cooperative PRMT5 inhibitor with IC50 of 9 nM in SDMA in-cell western assay, binds the PRMT5·MTA complex, selectively kills MTAP-deleted (MTAP-null) cells.
TNG908 binds apo-PRMT5 with a KD of 1.9 nM, and to the PRMT5·MTA complex with Kd of 0.3 nM in FA assays, 6-fold increase in potency in the presence of MTA.
TNG908 is 15-fold selective for MTAP-null cells relative to isogenic MTAP WT cells
TNG908 treatment (10, 30, or 60 mg/kg BID) drives dose-dependent PD and antitumor activity in the LN18 MTAP-null GBM xenograft model, exhibits strong, dose-dependent antitumor activity including a 48% tumor regression at the 120 mg/kg BID dose level in the LU99 MTAP-null NSCLC CDX model.
