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INK1117

Catalog No.
C3103
PI3Kα inhibitor
Grouped product items
SizePriceStock Qty
5mg
$166.00
Ship with 5-10 days
10mg
$291.00
Ship with 5-10 days
25mg
$638.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: 15nM: inhibits phosphoinositide 3-kinase α (PI3Kα) in vitro.

INK1117 is a novel, potent and selective inhibitor of PI3Kα with potential antineoplastic activity, which may induce tumor cell apoptosis and growth inhibition in PI3Kα-expressing tumor cells. INK1117 dampens signaling to Akt and suppresses the growth of cancer cells harboring wild-type or mutated p110α. PI3Ks, a family of eight lipid kinase enzymes, produce 3-phosphorylated phosphoinositides in cellular membranes and are promising targets for therapeutic development in cancer.

In vitro: INK1117 blocked class I PI3K enzymes (p110α, p110β, p110γ or p110δ) in the low to mid-nanomolar range in human natural killer (NK) cell lines. INK1117 selectively inhibited PI3K signaling in cellular assays when used at 0.1-1 μM. INK1117 selectively dampened p110 α when used at 1 μM. INK1117 did not inhibit production of IFN-γ protein in cells with anti-NKG2D, indicating that INK1117 did not decrease IFN-γ mRNA [1].

In vivo: Female C57BL/6 mice were orally given INK1117 at a dose of 60 mg/kg using a sterile disposable 20G-1.5” feeding needle. After 8 days, INK1117 had negligible effects on NK cell maturation or survival. However, INK1117 did not show significantly decrease in the percentage of B cells and did not alter the percentages of T cells or the fractions of CD4 and CD8 T cells, the percentages of NK cells in bone marrow and spleen [1].

Reference:
[1].  Yea, S., So, L., Mallya, S., Lee, J., Rajasekaran, K., Malarkannan, S., & Fruman, D. Effects of Novel Isoform-Selective Phosphoinositide 3-Kinase Inhibitors on Natural Killer Cell Function. Plos ONE. 2014; 9(6): e99486.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt363.4
Cas No.1268454-23-4
FormulaC19H17N5O3
SynonymsMLN1117,TAK-117
Solubility≤1mg/ml in DMSO;0.25mg/ml in dimethyl formamide
Chemical Name[6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-methanone
SDFDownload SDF
Canonical SMILESNC1=NC2=CC(C(C=C3)=CN4C3=NC=C4C(N5CCOCC5)=O)=CC=C2O1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

INK1117