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.