A potent inhibitor of PI3K isoforms (Kis = 19

GSK2126458 – 10 mg

Brand:
Cayman
CAS:
1086062-66-9
Storage:
-20
UN-No:
Non-Hazardous - /

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively).{20675} It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110α.{20675} GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models.{20675} GSK2126458 positively combines with inhibitors of discoidin domain receptor 1 (DDR1) inhibitor DDR1-IN-1 (Item No. 18092) to suppress the growth of SNU-1040 colorectal cancer cells.{29876}  

 

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Description

A potent inhibitor of PI3K isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively); also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively); orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models,

Formal name: 2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-benzenesulfonamide

Synonyms:  GSK458|Omipalisib

Molecular weight: 505.5

CAS: 1086062-66-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|mTOR||Product Type|Biochemicals|Kinase Inhibitors|PI3K||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling

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