AZD2281

Gilteritinib (ASP2215) is a potent FLT3/AXL inhibitor, showing strong anti-leukemic activity against AML (Acute Myeloid Leukemia) by acting on either or both FLT3-ITD and FLT3-D835 mutations. In vitro at 1 nM concentration, among the 78 tyrosine kinases tested, it hits FLT3, LTK, ALK, and AXL kinases by over 50% with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT, the inhibition of which is linked to a potential risk of myelosuppression. It inhibited the growth of MV4-11 cells harboring FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with the inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. ASP2215 decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells. It is in clinical evaluation for treatment of AML.

Soluble in DMSO