UNC5293 (C09-1184-146)

UNC5293 is a MERTK -selective and potent inhibitor ( K i =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 researchIn VitroUNC5293 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 less potent against FLT3, with an IC 50 of 170 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoUNC5293 (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 C max and AUC last are 9.2 μM and 2.5 h*μM, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:Viscous liquidIC50& Target:Ki: 190 pM (MERTK) IC50: 0.9 nM (MERTK). Specification: 0.99 Molecular Formula: C30H42N6O2 Molecular Weight: 518.69 PubChem CID: 146403042 Isomeric SMILES: CCC[C@H](C)NC1=NC=C2C(=CN(C2=N1)C3CCC(CC3)O)C4CCN(CC4)C(=O)C5=CC(=NC(=C5)C)C