Catalog # Availability Size / Price Qty
DCLK1-IN-1 | CAS No. 2222635-15-4 | Other Kinase Inhibitors
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Description: Potent and selective doublecortin like kinase 1/2 (DCLK1/2) inhibitor; orally bioavailable

Chemical Name: 5,11-Dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-5-(2,2,2-trifluoroethyl)-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

Purity: ≥98%

Product Details

Biological Activity

DCLK1-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.

External Portal Information 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.

Technical Data

Soluble to 100 mM in DMSO and to 100 mM in ethanol
Store at -20°C

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.

Additional Information

Licensing Caveats:
Sold under license from Dana-Farber Cancer Institute

Background References

  1. Discovery of a selective inhibitor of doublecortin like kinase 1.
    Ferguson et al.
    Nat.Chem.Biol., 2020;16:635

Product Datasheets

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