| Identification | Back Directory | [Name]
INK1117 | [CAS]
1268454-23-4 | [Synonyms]
TAK117
TAK-117
CS-2200
MLN1117
TAK 117
SerabeL
Serabelisib
INK-1117 MLN1117
MLN1117 (INK1117)
Serabelisib (MLN1117)
Serabelisib(INK-1117)
MLN1117 (Serabelisib)
Serabelisib (TAK-117)
TAK-117(INK1117,MLN1117)
Serabelisib(TAK-117,INK1117,MLN1117)
Serabelisib,MLN1117,INK1117, TAK-117
[6-(2-Amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinylmethanone
5-[3-(Morpholine-4-carbonyl)imidazo[1,2-a]pyridin-6-yl]-1,3-benzoxazol-2-amine
Methanone, [6-(2-aMino-5-benzoxazolyl)iMidazo[1,2-a]pyridin-3-yl]-4-Morpholinyl-
INK1117; INK-1117; INK 1117; MLN1117; MLN 1117; MLN-1117; TAK-117; TAK 117; TAK117
[6-(2-amino-1,3-benzoxazol-5-yl)imidazo[1,2-a]pyridin-3-yl]-morpholin-4-ylmethanone
methyl 6-((5-((3-(trifluoromethyl)phenyl)carbamoyl)naphthalen-2-yl)oxy)pyrimidine-4-carboxylate | [Molecular Formula]
C19H17N5O3 | [MOL File]
1268454-23-4.mol | [Molecular Weight]
363.37 |
| Chemical Properties | Back Directory | [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) | [color ]
White to gray |
| Hazard Information | Back Directory | [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] | [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. | [storage]
Store at -20°C | [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. |
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