INK1117 Property

Density 

1.55±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≤1mg/ml in DMSO;0.25mg/ml in dimethyl formamide

form 

crystalline solid

pka

4.75±0.50(Predicted)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

INK1117 Chemical Properties,Usage,Production

Uses

INK1117 is an inhibitor of phosphoinositide 3-kinase α (PI3Kα) that is selective for p110α in vitro (IC50 = 15 nM for PI3Kα vs. >1 μM for other isoforms, as well as for mTOR) and in cells when used at 1 μM. It blocks signaling to Akt and inhibits growth of cancer cells harboring wild-type or mutated p110α. INK1117 does not interfere with B cell proliferation or NK cell maturation and survival.[Cayman Chemical]

Uses

MLN 1117 is an inhibitor of PI3Kα which is selective for p110α in vitro. Useful in the attenuation of cell proliferation.

Biological Activity

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].

IC 50

15nm: inhibits phosphoinositide 3-kinase α (pi3kα) in vitro.

References

[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.