2281803-28-7

2281803-28-7 structure

Name: MEK/PI3K-IN-1
Chemical Name: MEK/PI3K-IN-1
CAS Number: 2281803-28-7
Molecular Formula: C₃₆H₃₇F₅IN₉O₆
Molecular Weight: 913.63
Catalog: Signaling Pathways Cell Cycle/DNA Damage PERK
Create Date: 2022-06-27 18:17:51
Modify Date: 2024-01-09 23:12:24
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].

Name	MEK/PI3K-IN-1

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.

Molecular Formula	C₃₆H₃₇F₅IN₉O₆
Molecular Weight	913.63