Chemical Structure : TNG456
CAS No.:
2962087-36-9
TNG456
(TNG-456)
Catalog No.: PC-26787Not For Human Use, Lab Use Only.
TNG456 is a potent, highly selective, brain-penetrant MTA-cooperative PRMT5 inhibitor with Ki,app of <2 pM, exhibits viability growth inhibition with GI50 of 20 nM for HAP1 MTAP-null cells, 50-fold selective over HAP1 MTAP WT cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TNG456 is a potent, highly selective, brain-penetrant MTA-cooperative PRMT5 inhibitor with Ki,app of <2 pM, exhibits viability growth inhibition with GI50 of 20 nM for HAP1 MTAP-null cells, 50-fold selective over HAP1 MTAP WT cells.
TNG456 shows no significant activity against a panel of 40 methyltransferases at 10 uM.
TNG456 (3, 10, 30, or 90 mg/kg BID) shows strong antitumor efficacy in U87MG MTAP-null GBM xenograft model, decreases SDMA-modified protein levels.
TNG456 exerts potent, on-target, and dose-dependent antitumor activity across diverse MTAP-deleted models representing multiple tumor histologies including CNS malignancies.
Physicochemical Properties
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M.Wt
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406.37
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Formula
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C18H17F3N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-N1-(4-Amino-1H-pyrazolo[4,3-c]pyridin-7-yl)-N2-methyl-N2-(1-(4-(trifluoromethyl)phenyl)ethyl)oxalamide
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References
1. Cottrell KM, et al. J Med Chem. 2026 May 18. doi: 10.1021/acs.jmedchem.6c00035.
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