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Chemical Structure : TNG260
Catalog No.: 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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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.
| M.Wt | 383.44 | |
| Formula | C20H18FN3O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Leanne Ahronian, et al. BMJ Journal Volume 10, Issue Suppl 2
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