1086062-66-9
1086062-66-9
Chemical Structure
Omipalisib
Synonym(s): GSK2126458; GSK458
- CAS No.: 1086062-66-9
- Formula:C25H17F2N5O3S
- Molecular Weight:505.50
IUPAC Name: 2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide
InChIKey: CGBJSGAELGCMKE-UHFFFAOYSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Omipalisib | 99.94% | 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. | ||||||||||||||||||||
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Omipalisib (Standard) | ≥98% | Omipalisib (Standard) is the analytical standard of Omipalisib (HY-10297). This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
