Omipalisib
Omipalisib (GSK2126458) is an orally active and highly selective inhibitor of PI3K with Kis of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2, respectively. Omipalisib has anti-cancer activity[1][2][3].
Product Specifications
CAS Number
1086062-66-9
Product Name Alternative
GSK2126458; GSK458
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Autophagy; mTOR; PI3K
Type
Reference compound
Related Pathways
Autophagy; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/GSK2126458.html
Concentration
10mM
Purity
99.94
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
COC1=NC=C(C=C1NS(C2=CC=C(C=C2F)F)(=O)=O)C3=CC=C(C4=C3)N=CC=C4C5=CN=NC=C5
Molecular Formula
C25H17F2N5O3S
Molecular Weight
505.50
Precautions
H302, H315, H319, H335
References & Citations
[1]Knight SD, et al. Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin. ACS Med. Chem. Lett. 2010, 1 (1), 39-43.|[2]Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther. 2012 Apr;11 (4) :909-20.|[3]Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8 (10) :2145-50.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
MTORC1; mTORC2; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
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