Chemical Structure : TSL2109
CAS No.:
2619847-12-8
TSL2109
(TSL-2109)
Catalog No.: PC-26150Not For Human Use, Lab Use Only.
TSL2109 is a potent, selective, orally active Dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) inhibitor with IC50 of 22 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TSL2109 is a potent, selective, orally active Dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) inhibitor with IC50 of 22 nM.
TSL2109 displays potent inhibitory activity against DYRK2 at 1 uM, while exhibiting <50% inhibition against over 93% of a panel of 416 kinases.
TSL2109 effectively occupies the ATP-binding pocket of DYRK2.
TSL2109 exhibits potent antiproliferative activity (IC50=0.933 μM) and dose-dependent cell growth inhibitory activity against PCa DU145 cells.
TSL2109 significantly inhibits the E2F TARGETS and G2M CHECKPOINT pathways, both closely associated with cell cycle progression, significantly upregulates APOPTOSIS and P53 pathways.
TSL2109 (100-200 mg/kg) produced marked antitumor effects in the DU145 xenograft models.
TSL2109 exerted significant inhibitory effects against enzalutamide-resistant 22Rv1 cells and xenografts.
Physicochemical Properties
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M.Wt
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548.69
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Formula
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C28H33FN8OS
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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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(6-((4-(2-(Diethylamino)benzo[d]thiazol-6-yl)-5-fluoropyrimidin-2-yl)amino)pyridin-3-yl)(4-isopropylpiperazin-1-yl)methanone
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References
1. Kai Yuan, et al. J Med Chem. 2025 Dec 25;68(24):25783-25793.
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