DCLK1-IN-1

Name: DCLK1-IN-1
Brand: Tocris Bioscience
SKU: 7285

Tocris Bioscience, part of Bio-Techne | Catalog # 7285

COA / SDS

Potent and selective doublecortin like kinase 1/2 (DCLK1/2) inhibitor; orally bioavailable

Key Product Details

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)
Molecular Weight:	527.55

View Full Technical Details for DCLK1-IN-1

Technical Data
Citations

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

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.

External Portal Information

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.

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
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.

Solubility for DCLK1-IN-1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.90 mL	9.48 mL	18.96 mL
5 mM	0.38 mL	1.90 mL	3.79 mL
10 mM	0.19 mL	0.95 mL	1.90 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 Discovery of a selective inhibitor of doublecortin like kinase 1. Nat.Chem.Biol. 2020 PMID: 32251410