GSK2126458 CAS: 1086062-66-9
MF: C25H17F2N5O3S
MW: 505.50
An inhibitor of p110 mutants.

GSK2126458 (CAS 1086062-66-9)

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Alternate Names: 2,4-difluoro-N-(2-(methyloxy)-5-(4-(4-pyridazinyl)-6-quinolinyl)-3-pyridinyl)benzenesulfonamide
Application: GSK2126458 is an inhibitor of p110 mutants
CAS Number: 1086062-66-9
Purity: ≥98%
Molecular Weight: 505.50
Molecular Formula: C25H17F2N5O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).

GSK2126458 is a potent inhibitor of common activating mutants of p110α (E542K, E545K, and H1047R), with Ki values of 8 pM, 8 pM and 9 pM, respectively. GSK2126458 causes a significant reduction in the levels of pAkt-S473 in T47D and BT474 cells with an IC50 of 0.41 nM and 0.18 nM, respectively. GSK2126458 leads to a G1 cell cycle arrest and produces the inhibitory effect on cell proliferation in a large panel of cell lines, including T47D and BT474 breast cancer lines with IC50 of 3 nM and 2.4 nM, respectively. GSK2126458 is an inhibitor of mTOR, PI 3-kinase p110 α, PI 3-kinase p110 β, PI 3-kinase p110 δ and PI 3-kinase p110 γ.

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
Storage :
Store at -20° C
Boiling Point :
715.59 °C at 760 mmHg (Predicted)
Density :
1.45 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
Ki Data :
p110α: Ki= 0.02 nM; p110δ: Ki= 0.02 nM; p110γ: Ki= 0.06 nM; p110β: Ki= 0.13 nM; mTORC1: Ki= 0.18 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
25167777
MDL Number :
MFCD16038929
SMILES :
COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C4=CN=NC=C4)NS(=O)(=O)C5=C(C=C(C=C5)F)F

Download SDS (MSDS)

Certificate of Analysis

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