FLT3-IN-11

Names

[ CAS No. ]:
2499966-50-4

[ Name ]:
FLT3-IN-11

Biological Activity

[Description]:

FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3

[Target]

IC50: 7.22 nM (wild-type FLT3) and 4.95 nM (FLT3-D835Y)[1]


[In Vitro]

FLT3-IN-11 (compound 30) efficiently inhibits the growth of multiple mutant BaF3 cells expressing FLT3-ITD, FLT3-D835V/F, FLT3-F691L, FLT3-ITD-F691L, and FLT3-ITD-D835Y[1].

[In Vivo]

Oral administration of FLT3-IN-11 (compound 30) at 6 mg/kg/d could significantly suppress tumor growth in the MV4-11 cell-inoculated xenograft model, exhibiting tumor growth inhibitory rates of 83.5%[1].

[References]

[1]. Lexian Tong, et al. Identification of 2-Aminopyrimidine Derivatives as FLT3 Kinase Inhibitors with High Selectivity over c-KIT. J Med Chem. 2022 Feb 24;65(4):3229-3248.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H25F3N6O

[ Molecular Weight ]:
422.45

Related Compounds