UNC5293 是一种有效的、口服的、高度MERTK选择性的抑制剂 (Ki=190 pM)。UNC5293 抑制 MERTK (IC50=0.9 nM)，对 Axl、Tyro3 和 FLT3 更具选择性。UNC5293 表现出优异的小鼠药代动力学特性，并可以被用于骨髓白血病研究。

UNC5293 is a potent, orally available and highly MERTK-selective inhibitor with Ki of 190 pM. UNC5293 inhibits MERTK ( IC 50 =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 [1].

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 IC 50 of 9.4 nM. In the SEM B-ALL cell line, UNC5293 is weak against FLT3, with an IC 50 of 170 nM [1].

UNC5293 (oral administration; 120 mg/kg; single dose) effectively inhibit MERTK in vivo in orthotopic 697 B-ALL mice xenografts [1].UNC5293 (oral gavage; 3 mg/kg; single dose) exhibits excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the C max and AUC last are 9.2 μM and 2.5 h*μM, respectively [1].

2226789-82-6

C30H42N6O2

518.69

UNC5293

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years