AZD 7507

FMS抑制剂(IC50=3nM)；1µM时对FMS的选择性优于c-KIT、ARK-5、FLT4、RSK1和77种其他激酶；100nM时诱导分离的Fms+小鼠骨髓细胞凋亡，但不诱导Fms-小鼠骨髓细胞凋亡；以每天100mg/kg的剂量降低肿瘤相关Fms+巨噬细胞的水平，增加肿瘤相关CD8+T细胞的数量，减轻肿瘤重量，并增加UN-KPC-960小鼠PDAC模型中的存活率；降低分离的UN-KPC-960肿瘤中的α-Sma并增加E-cadherin水平；降低分离的UN-KPC-960肿瘤蛋白裂解物中的Ifn-γ、Il-10、Il-17A、Cxcl2、Ccl2、Ccl7和Ccl12水平。An FMS inhibitor (IC50 = 3 nM); selective for FMS over c-KIT, ARK-5, FLT4, RSK1, and 77 other kinases at 1 µM; induces apoptosis in isolated Fms+ mouse bone marrow cells but not Fms- mouse bone marrow cells at 100 nM; 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 PDAC at 100 mg/kg per day; decreases α-Sma and increases E-cadherin levels on isolated UN-KPC-960 tumors; reduces the levels of Ifn-γ, Il-10, Il-17A, Cxcl2, Ccl2, Ccl7, and Ccl12 in protein lysates from isolated UN-KPC-960 tumors.分子式C23H27FN6O3分子量454.5O=C(C1=C(NC2=CC=C(C)C=C2F)C3=C(C=C(C(N4CCN(CC4)CCO)=C3)OC)N=N1)N