A multi-kinase inhibitor
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LMTK3 Inhibitor C28

Item No. 41877

Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-(4-pyridinyl)-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazine
CAS Number
2764850-23-7
Synonyms
  • Lemur Tyrosine Kinase-IN-C28
  • Lemur Tyrosine Kinase 3 Inhibitor 1
  • Lemur Tyrosine Kinase Inhibitor C28
  • LMTK3-IN-1
  • LMTK3-IN-C28
  • LMTK3 Inhibitor 1
Molecular Formula
C18H11F3N4O
Formula Weight
356.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
FC(F)(OC1=CC=CC(C2=CN=C3C=CC(C4=CC=NC=C4)=NN32)=C1)F
InChi Code
InChI=1S/C18H11F3N4O/c19-18(20,21)26-14-3-1-2-13(10-14)16-11-23-17-5-4-15(24-25(16)17)12-6-8-22-9-7-12/h1-11H
InChi Key
SFBZOJORTROAIE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    LMTK3 inhibitor C28 is a multi-kinase inhibitor.1 It inhibits lemur tyrosine kinase 3 (LMTK3), CDC-like kinase 2 (Clk2), dual-specificity tyrosine phosphorylation-regulated kinase 1α (DYRK1α), homeodomain-interacting protein kinase 2 (HIPK2), and IL-1 receptor-associated kinase 4 (IRAK4; IC50s = 67, 5, 6, 48, and 41 nM, respectively), among others. LMTK3 inhibitor C28 is selective for these kinases over a panel of 122 kinases at 1 µM. It induces proteasomal degradation of LMTK3 in MCF-7, T47D, and MDA-MB-231 breast cancer cells when used at concentrations of 5 or 10 µM. LMTK3 inhibitor C28 (10 µM) reduces the levels of IRAK4, estrogen receptor α (ERα), phosphorylated tropomyosin-related kinase A (TrkA), and HIPK2 in T47D cells. It induces induces apoptosis in MCF-7, T47D, and MDA-MB-231 cells when used at a concentration of 10 µM. In vivo, LMTK3 inhibitor C28 (10 mg/kg per day) reduces tumor growth and volume in an MDA-MB-231 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ditsiou, A., Cilibrasi, C., Simigdala, N., et al. The structure-function relationship of oncogenic LMTK3. Sci. Adv. 6(46), eabc3099 (2020).