GSK 1059615A potent inhibitor of PI 3-kinase and FRAP (mTOR)

GSK 1059615 (CAS 958852-01-2)

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Application: A potent inhibitor of PI 3-kinase and FRAP (mTOR)
CAS Number: 958852-01-2
Molecular Weight: 333.36
Molecular Formula: C18H11N3O2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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GSK 1059615, a pyridinylquinoline derivative, is a novel, ATP-competitive, and reversible class I PI 3-kinase inhibitor. GSK 1059615 inhibits PI 3-kinase signaling and induces G1 arrest and apoptosis, especially in breast tumor cells. GSK 1059615 inhibits PI 3-kinase α (IC50 of 2 nM, Ki of 0.42 nM), β (Ki of 0.6 nM), γ (Ki of 0.47 nM) and δ (Ki of 1.7 nM). GSK 1059615 is also an inhibitor of mTOR (FRAP) (IC50 of 0.4-12 nM).

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in DMSO (10 mM), DMSO:PBS(pH 7.2) 1:1 (0.5 mg/ml), water (<1 mg/ml), ethanol (<1 mg/ml), and DMF (0.25 mg/ml).
Storage :
Store at 4° C
Density :
1.44 g/cm3 (Predicted)
Refractive Index :
n20D 1.76 (Predicted)
IC50 :
PI3Kα: IC50 = 0.4 nM; PI3Kβ: IC50 = 0.6 nM; PI3Kδ: IC50 = 2 nM; PI3Kγ: IC50 = 5 nM; mTOR: IC50 = 12 nM; Inhibits the phosphorylation of Akt at S473: IC50 = 40 nM (T47D and BT474 cancer cells)
Ki Data :
PI3Kα: Ki= 0.42 nM; PI3Kβ: Ki= 0.6 nM; PI3Kγ: Ki= 0.47 nM; PI3Kδ: Ki= 1.7 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
23582824
MDL Number :
MFCD18074517
SMILES :
C1=CC2=NC=CC(=C2C=C1/C=C\3/C(=O)NC(=O)S3)C4=CC=NC=C4

Download SDS (MSDS)

Certificate of Analysis

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