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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-TNG908
TNG908

Chemical Structure : TNG908

CAS No.: 2760481-53-4

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TNG908 (Ralometostat, TNG-908)

货号: 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.

规格 价格 库存 数量
2 mg ￥1980 In stock
5 mg ￥3280 In stock
10 mg ￥5280 In stock
25 mg ￥8580 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 409.51
分子式 C21H23N5O2S
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

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

参考文献

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

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