TNG456 (TNG-456)

Chemical Structure : TNG456

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	406.37
分子式	C18H17F3N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-N1-(4-Amino-1H-pyrazolo[4,3-c]pyridin-7-yl)-N2-methyl-N2-(1-(4-(trifluoromethyl)phenyl)ethyl)oxalamide

参考文献

1. Cottrell KM, et al. J Med Chem. 2026 May 18. doi: 10.1021/acs.jmedchem.6c00035.

TNG456 (TNG-456)

生物&药学活性

物理化学性质&存储条件

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TNG456 (TNG-456)

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物理化学性质&存储条件

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