| Name | DCLK1-IN-1 |
| Description | DCLK1-IN-1 is a selective, in vivo compatible chemical probe of the kinase domain of doublecortin-like kinase 1 (DCLK1) and a highly selective DCLK1/2 inhibitor with IC50 values of 9.5/57.2 nM (DCLK1) and 31/103 nM (DCLK2) by binding and kinase assays, respectively. It has low toxicity and is used to study DCLK1 biology and determine its role in cancer. |
| In vitro | METHODS: A NanoBRET tracer (TAE684-NanoBRET-590) was synthesized and a DCLK1 NanoBRET assay was developed to measure the effect of DCLK1-IN-1 on cell proliferation in HCT116 cells.
RESULTS The IC50 value of DCLK1-IN-1 against HCT116 cells was 279nM. [1]
METHODS: ACHN, 786-O, and CAKI-1 RCC cells were treated with DCLK1-IN-1 (0.5, 1, 5, 10 μM) and subjected to wound healing assays.
RESULTS DCLK1-IN-1 exerted a significant anti-migratory effect on ACHN, 786-O, and CAKI-1 RCC cells, with ACHN and CAKI-1 cells showing a typical dose-dependent decrease in wound healing from 0.5 to 10 μM, while 786-O cells showed a significant decrease at a dose of 10 μM. [2] |
| In vivo | DCLK1-IN-1 (3 mg/kg, intravenous injection; 10 mg/kg, oral administration) has good pharmacokinetic characteristics in mice, with a half-life of 2.09 hours, an area under the curve (AUCinf) of 5506 hr*ng/mL, and an oral bioavailability of 81%. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | 2% DMSO+40% PEG300+5% Tween 80+53% Saline : 1 mg/mL, Sonication is recommended.Working solution is recommended to be prepared and used immediately.
DMSO : 50 mg/mL (94.78 mM), Sonication is recommended.
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| Keywords | DCLK1 IN 1 | DCLK1-IN-1 | signaling | PDAC | KRAS | cancer | low | ERK | Inhibitor | selective | DCLK1IN1 | inhibit | DCLK-1-IN-1 | toxicity |
| Related Compound Libraries | 经典已知活性库 | 激酶抑制剂库 | NO PAINS 化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌活性化合物库 |
United States
