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首页-小分子抑制剂&激动剂-Tyrosine Kinase-DYRK-TSL2109
TSL2109

Chemical Structure : TSL2109

CAS No.: 2619847-12-8

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TSL2109 (TSL-2109)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 548.69
分子式 C28H33FN8OS
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

(6-((4-(2-(Diethylamino)benzo[d]thiazol-6-yl)-5-fluoropyrimidin-2-yl)amino)pyridin-3-yl)(4-isopropylpiperazin-1-yl)methanone

参考文献

1. Kai Yuan, et al. J Med Chem. 2025 Dec 25;68(24):25783-25793.

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