产品
编 号:F749989
分子式:C30H42N6O2
分子量:518.69
产品类型
结构图
CAS No: 2226789-82-6
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产品详情
生物活性:
UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research.
体内研究:
UNC5293 (oral administration; 120?mg/kg; single dose) effectively inhibit MERTK?in?vivo in orthotopic 697?B-ALL mice xenografts.UNC5293 (oral gavage; 3 mg/kg; single dose) has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the Cmax and AUClast are 9.2 μM and 2.5 h*μM, respectively.
体外研究:
UNC5293?provides selective target inhibition in cell-based assays. In cultures of the human B-cell?acute lymphoblastic leukemia?(B-ALL) cell line,?UNC5293 inhibits phosphorylation of MERTK with an IC50?of 9.4?nM.?In the SEM B-ALL cell line, UNC5293 is less potent against FLT3, with an IC50?of 170?nM.