MEK/PI3K-IN-1

Names

[ CAS No. ]:
2281803-28-7

[ Name ]:
MEK/PI3K-IN-1

Biological Activity

[Description]:

MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> MAPK/ERK Pathway >> MEK
Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Signaling Pathways >> Cell Cycle/DNA Damage >> PERK

[Target]

MEK1:124 ± 11 nM (IC50)

PI3Kα:130 ± 13 nM (IC50)

PI3Kδ:236 ± 29 nM (IC50)

PI3Kβ:1537 ± 188 nM (IC50)

PI3Kγ:2745 ± 485 nM (IC50)


[References]

[1]. Van Dort ME, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

Chemical & Physical Properties

[ Molecular Formula ]:
C36H37F5IN9O6

[ Molecular Weight ]:
913.63

Related Compounds