A potent pan-PI3K and mTOR inhibitor
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GSK2126458

Item No. 17377

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,4-difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]-benzenesulfonamide
CAS Number
1086062-66-9
Synonyms
  • GSK458
  • Omipalisib
Molecular Formula
C25H17F2N5O3S
Formula Weight
505.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
225, 300 nm
SMILES
COC1=C(NS(C2=CC=C(F)C=C2F)(=O)=O)C=C(C3=CC(C(C4=CC=NN=C4)=CC=N5)=C5C=C3)C=N1
InChi Code
InChI=1S/C25H17F2N5O3S/c1-35-25-23(32-36(33,34)24-5-3-18(26)12-21(24)27)11-17(13-29-25)15-2-4-22-20(10-15)19(7-8-28-22)16-6-9-30-31-14-16/h2-14,32H,1H3
InChi Key
CGBJSGAELGCMKE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $238

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    10 mg

    $418

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    50 mg

    $1,303

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    Product Description

    GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase isoforms (Kis = 19, 130, 24, and 60 pM for p110α, β, δ, and γ, respectively).1 It also inhibits mTOR in both mTORC1 and mTORC2 (Kis = 180 and 300 nM, respectively), as well as several common mutant forms of p110α.1 GSK2126458 is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models.1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Knight, S.D., Adams, N.D., Burgess, J.L., et al. Discovery of GSK2126458, a highly potent inhibitor of P13K and the mammalian target of rapamycin. ACS Med. Chem. Lett. 1(1), 39-43 (2010).

    2. Kim, H.G., Tan, L., Weisberg, E.L., et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 8(10), 2145-2150 (2013).