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Submit ReviewDCLK1-IN-1 is a potent and selective doublecortin like kinase 1/2 (DCLK1/2) inhibitor (IC50 values are DCLK1 =9.5 and 57.2 nM and DCLK2 = 31 and 103 nM in binding and kinase assay, respectively). Exhibits no significant activity against ERK5, ACK, BRD4 and LRRK2. Exhibits DCLK inhibition in pancreatic ductal adenocarcinoma (PDAC) organoid models. Orally bioavailable.
Sold under license from Dana-Farber Cancer Institute
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of DCLK1-IN-1 is reviewed on the chemical probes website.
DCLK1-IN-1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 527.55 |
Formula | C26H28F3N7O2 |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 2222635-15-4 |
PubChem ID | 134457640 |
InChI Key | OQFCHSFVWSLDAO-UHFFFAOYSA-N |
Smiles | COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C4N(C(C5=CC=CC=C5N(C4=N3)C)=O)CC(F)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 52.76 | 100 | |
ethanol | 52.76 | 100 |
The following data is based on the product molecular weight 527.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.9 mL | 9.48 mL | 18.96 mL |
5 mM | 0.38 mL | 1.9 mL | 3.79 mL |
10 mM | 0.19 mL | 0.95 mL | 1.9 mL |
50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
References are publications that support the biological activity of the product.
Ferguson et al (2020) Discovery of a selective inhibitor of doublecortin like kinase 1. Nat.Chem.Biol. 16 635 PMID: 32251410
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Keywords: DCLK1-IN-1, DCLK1-IN-1 supplier, Potent, selective, doublecortin, like, kinase, 1/2, DCLK1/2, DCLK1, DCLK2, inhibitors, inhibits, Other, Kinases, 7285, Tocris Bioscience
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