FLT3/D835Y-IN-1

FLT3/D835Y-IN-1 (compound 13a) is an orally active, selective inhibitor of FLT3 and FLT3/D835Y with IC50 values of 0.26 nM and 0.18 nM, respectively. It exhibits anticancer efficacy and has research value in AML (acute myeloid leukemia).

FLT3-ITD/D835Y-IN-1 (Compound 1) is an inhibitor of FLT3-ITD and BCR-ABL. It induces pro-apoptotic (apoptosis) effects by inhibiting the FLT3 and BCR-ABL pathways, along with potentially other targets. This compound is applicable in acute myeloid leukemia (AML) research.

FLT3D835Y/F691L-IN-1 (compd 8v) is an orally active inhibitor targeting the secondary mutations D835Y/F691L in the FLT3 tyrosine kinase domain, with IC50 values of 1.5 and 9.7 nM, respectively. This compound is applicable in research related to acute myeloid leukemia.

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM for FLT3 and 0.199 nM for the FLT3/D835Y mutant. It demonstrates significant antiproliferative effects against MV4-11 cells and Ba/F3 cell lines expressing mutant FLT kinase variants, including FLT-D835Y and FLT3-F691L [1].

FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC50 values of 1 nM for FLT3-D835Y and 4 nM for FLT3-ITD. It shows anti-proliferative effects on FLT3-ITD-positive AML cell lines, with IC50s of 7 nM in MV4-11, 9 nM in MOLM-13, and 4 nM in a MOLM-13 variant harboring the FLT3-ITD-D835Y mutation. FLT3-IN-20 is utilized in cancer research [1].

Pacritinib (SB1518) citrate effectively inhibits wild-type JAK2 (IC 50 =23 nM) and the JAK2 V617F mutant (IC 50 =19 nM). It also targets FLT3 (IC 50 =22 nM) and the FLT3 D835Y mutant (IC 50 =6 nM). This compound is utilized in the study of acute myeloid leukemia (AML) and myelofibrosis (MF) [1] [2] [3].