TNG260 | CoreDAC inhibitor | Probechem Biochemicals

Chemical Structure : TNG260

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TNG260 (TNG-260, TNG 260)

货号: PC-20671Not For Human Use, Lab Use Only.

TNG260 (TNG-260) is a potent, CoREST-selective deacetylase (CoreDAC) inhibitor, inhibits HDAC1 with 10-fold selectivity over HDAC3 in cells.

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生物&药学活性

TNG260 (TNG-260) is a potent, CoREST-selective deacetylase (CoreDAC) inhibitor, inhibits HDAC1 with 10-fold selectivity over HDAC3 in cells.
TNG260 displays 500-fold selectivity for the CoREST complex over the other HDAC1-containing complexes, NuRD and Sin3.
TNG260 re-sensitizes α-PD1 resistant STK11-mutant MC38 syngeneic tumor model with α-PD1.
The combination of TNG260 and α-PD1 led to durable complete tumor regressions in α-PD1 resistant STK11-mutant MC38 syngeneic tumor models.
TNG260 has no anti-tumor efficacy in immunocompromised mice, indicating the tumor cell killing with TNG260 is immune-mediated and not due to direct cell killing.
TNG260 also decreased intratumoral infiltration of neutrophils, an immune suppressive cell type associated with STK11-mutant NSCLC.
TNG260 reverses the immune evasion phenotype caused by loss of STK11 and induces tumor regressions in an STK11-mutant model in combination with α-PD1.

物理化学性质&存储条件

分子量	383.44
分子式	C20H18FN3O2S
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	NC1=CC=C(C2=CC=C(F)C=C2)C=C1NC(C3=CC=C([S@](=O)(C)=N)C=C3)=O

参考文献

1. Leanne Ahronian, et al. BMJ Journal Volume 10, Issue Suppl 2

TNG260 (TNG-260, TNG 260)

生物&药学活性

物理化学性质&存储条件

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TNG260 (TNG-260, TNG 260)

生物&药学活性

物理化学性质&存储条件

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