JAK3/BTK-IN-6

Names

[ CAS No. ]:
2243136-03-8

[ Name ]:
JAK3/BTK-IN-6

Biological Activity

[Description]:

JAK3/BTK-IN-6 (compound 14h) is a potent BTK and JAK3 dual inhibitor, with IC50 values of 0.6 and 0.4 nM, respectively. JAK3/BTK-IN-6 shows good metabolic stability in human liver microsome. JAK3/BTK-IN-6 can be used for hematological and immune diseases research[1].

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> JAK
Signaling Pathways >> Epigenetics >> JAK
Signaling Pathways >> Stem Cell/Wnt >> JAK
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

[Target]

JAK3:0.4 nM (IC50)

JAK2:657.9 nM (IC50)

JAK1:>1000 nM (IC50)

Tyk2:>1000 nM (IC50)


[In Vitro]

JAK3/BTK-IN-6 (compound 14h) shows antiproliferative activities against hematopoietic cells (Raji, Romas, HEL, Jeko-1, and OCI-LY10), with IC50 values of 1.7, 0.5, 1.1, 0.5, and 1-10, respectively[1].

[References]

[1]. Ren J, et al. Design and synthesis of boron-containing diphenylpyrimidines as potent BTK and JAK3 dual inhibitors. Bioorg Med Chem. 2020 Jan 15;28(2):115236.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H17BF3N5O3

[ Molecular Weight ]:
455.20

Related Compounds