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描述 | DCLK1-IN-1 is a selective chemical probe with oral bioavailability and in vivo compatibility, targeting the doublecortin like kinase 1 (DCLK1 kinase) domain. It inhibits both DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assays, respectively). DCLK1-IN-1 demonstrates low toxicity, enabling investigation into DCLK1 biology and its role in cancers such as DCLK1+ pancreatic ductal adenocarcinoma (PDAC) [1]. |
体内研究 | DCLK1-IN-1 exhibits promising pharmacokinetics in mice, characterized by a half-life of 2.09 hours, an area under the curve of 5506 h/ng/mL, and 81% oral bioavailability [1]. |
体外研究 | DCLK1-IN-1 exhibits negligible activity against ERK5, ACK, and LRRK2. It demonstrates potent binding to DCLK1 in HCT116 cells (IC50=279 nM). In PATU-8988T cell lysates and live cells, DCLK1-IN-1 significantly inhibits DCLK1 and weakly inhibits ERK5 [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.90mL 0.38mL 0.19mL |
9.48mL 1.90mL 0.95mL |
18.96mL 3.79mL 1.90mL |
CAS号 | 2222635-15-4 |
分子式 | C26H28F3N7O2 |
分子量 | 527.541 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 35 mg/mL(66.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |