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TNG908

Chemical Structure : TNG908

CAS No.: 2760481-53-4

TNG908 (TNG-908)

Catalog No.: PC-22132Not For Human Use, Lab Use Only.

TNG908 (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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TNG908 (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.

Physicochemical Properties

M.Wt 409.51
Formula C21H23N5O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(6-Amino-5-methylpyridin-3-yl)-2-((2R,5S)-2-(benzo[d]thiazol-5-yl)-5-methylpiperidin-1-yl)-2-oxoacetamide

References

1. Cottrell KM, et al. J Med Chem. 2024 Apr 10. doi: 10.1021/acs.jmedchem.4c00133.

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