MEK/PI3K-IN-1
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].
Product Specifications
CAS Number
2281803-28-7
UNSPSC
12352005
Target
MEK; PERK; PI3K
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; MAPK/ERK Pathway; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/mek-pi3k-in-1.html
Solubility
10 mM in DMSO
Smiles
O=C(C1=C(C(F)=C(C=C1)F)NC2=CC=C(C=C2F)I)NOCCOCCOCCOCCNC3=NC(N4CCOCC4)=NC(N5C(C(F)F)=NC6=C5C=CC=C6)=N3
Molecular Formula
C36H37F5IN9O6
Molecular Weight
913.63
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MEK1; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
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