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Chemical Structure : TNG908
CAS No.: 2760481-53-4
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $398 | In stock | |
| 5 mg | $588 | In stock | |
| 10 mg | $958 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 409.51 | |
| Formula | C21H23N5O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Cottrell KM, et al. J Med Chem. 2024 Apr 10. doi: 10.1021/acs.jmedchem.4c00133.
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