产品描述:
AZD 7507 is an inhibitor of CSF-1 receptor tyrosine kinase (FMS; IC50 = 3 nM).{66520} It is selective for FMS over c-KIT, aurora kinase 5 (ARK-5), FMS-related tyrosine kinase 4 (FLT4), p90 ribosomal S6 kinase (RSK1), and 77 other kinases at 1 µM. AZD 7505 (100 nM) induces apoptosis in isolated Fms+ mouse bone marrow cells but not Fms- mouse bone marrow cells. In vivo, AZD 7505 (100 mg/kg per day) reduces the levels of tumor-associated Fms+ macrophages, increases the number of tumor-associated CD8+ T cells, decreases tumor weight, and increases survival in a UN-KPC-960 murine model of pancreatic ductal adenocarcinoma (PDAC). It decreases α-smooth muscle actin (α-Sma) levels and increases E-cadherin levels on isolated UN-KPC-960 tumor tissue, as well as reduces the levels of Ifn-γ, Il-10, Il-17a, chemokine (C-X-C motif) ligand 2 (Cxcl2), chemokine (C-C motif) ligand 2 (Ccl2), Ccl7, and Ccl12 in protein lysates from the same tumors.