Formulation: A solid
Formal Name: 6-(4-pyridinyl)-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazine
Purity: ≥98%
Formula Markup: C18H11F3N4O
Formula Weight: 356,3
Shelf life (days): 1460
CAS Number: 2764850-23-7
Notes: LMTK3 inhibitor C28 is a multi-kinase inhibitor.{69968} 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.
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