Pricing Availability   Qty
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% (HPLC)

Biological Activity for DCLK1-IN-1

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.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

External Portal Information for DCLK1-IN-1 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.

Compound Libraries for DCLK1-IN-1

DCLK1-IN-1 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for DCLK1-IN-1

M. Wt 527.55
Formula C26H28F3N7O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2222635-15-4
PubChem ID 134457640
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.

Solubility Data for DCLK1-IN-1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 52.76 100
ethanol 52.76 100

Preparing Stock Solutions for DCLK1-IN-1

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for DCLK1-IN-1

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

Citations for DCLK1-IN-1

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