DCLK1-IN-1

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Cat.No. 7285 - DCLK1-IN-1 | C26H28F3N7O2 | CAS No. 2222635-15-4
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)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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

Technical Data

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 Data

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

Preparing Stock Solutions

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

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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