An inhibitor of DCLK1
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DCLK1-IN-1

Item No. 40448

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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
CAS Number
2222635-15-4
Synonyms
  • DCLK1 Inhibitor 1
  • Doublecortin-like Kinase 1-IN-1
  • Doublecortin-like Kinase 1 Inhibitor 1
Molecular Formula
C26H28F3N7O2
Formula Weight
527.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
CN(C1=CC=CC=C1C2=O)C3=NC(NC(C=CC(N(CC4)CCN4C)=C5)=C5OC)=NC=C3N2CC(F)(F)F
InChi Code
InChI=1S/C26H28F3N7O2/c1-33-10-12-35(13-11-33)17-8-9-19(22(14-17)38-3)31-25-30-15-21-23(32-25)34(2)20-7-5-4-6-18(20)24(37)36(21)16-26(27,28)29/h4-9,14-15H,10-13,16H2,1-3H3,(H,30,31,32)
InChi Key
OQFCHSFVWSLDAO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $59

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    5 mg

    $263

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    10 mg

    $467

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    25 mg

    $1,021

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    Product Description

    DCLK1-IN-1 is an inhibitor of doublecortin-like kinase 1 (DCLK1; IC50 = 17 nM).1 It is selective for DCLK1 over leucine-rich repeat kinase 2 (LRRK2), bromodomain-containing protein 4 (BRD4), and ERK5 (IC50s = 7,000, >10,000, and 3,350 nM, respectively). DCLK1-IN-1 (1 µM) reduces the number of cells in primary patient-derived pancreatic cancer organoids. In vivo, DCLK1-IN-1 (10 mg/kg every other day) reduces plaque area and collagen levels in the aortic arches and serum levels of Tnf-α and Il-6 an ApoE-/- mouse model of atherosclerosis induced by a high-fat diet.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ferguson, F.M., Liu, Y., Harshbarger, W., et al. Synthesis and structure-activity relationships of DCLK1 kinase inhibitors based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold. J. Med. Chem. 63(14), 7817-7826 (2020).

    2. Huang, Z., Shen, S., Han, X., et al. Macrophage DCLK1 promotes atherosclerosis via binding to IKKβ and inducing inflammatory responses. EMBO Mol. Med. 15(5), e17198 (2023).