- INK1117
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- $1.00 / 1g
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2019-12-20
- CAS:1268454-23-4
- Min. Order: 1g
- Purity: 99.99%
- Supply Ability: 2tons
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| | INK1117 Basic information |
| Product Name: | INK1117 | | Synonyms: | Methanone, [6-(2-aMino-5-benzoxazolyl)iMidazo[1,2-a]pyridin-3-yl]-4-Morpholinyl-;INK-1117 MLN1117;MLN1117;MLN1117 (INK1117);[6-(2-Amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinylmethanone;[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;TAK-117(INK1117,MLN1117) | | CAS: | 1268454-23-4 | | MF: | C19H17N5O3 | | MW: | 363.37 | | EINECS: | | | Product Categories: | | | Mol File: | 1268454-23-4.mol |  |
| | INK1117 Chemical Properties |
| 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) |
| | INK1117 Usage And Synthesis |
| Uses | MLN 1117 is an inhibitor of PI3Kα which is selective for p110α in vitro. Useful in the attenuation of cell proliferation. | | 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. | | 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. |
| | INK1117 Preparation Products And Raw materials |
| Raw materials | Methanone, (6-?bromoimidazo[1,?2-?a]?pyridin-?3-?yl)?-?4-?morpholinyl--->5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2yl)benzo[d]oxazol-2-amine-->5-BROMOBENZO[D]OXAZOL-2-AMINE-->6-Bromoimidazo[1,2-a]pyridine-3-carboxylicacid-->(2-Aminobenzo[d]oxazol-5-yl)-boronic acid hydrochloride-->IMidazo[1,2-a]pyridine-3-carboxylic acid, 6-broMo-, ethyl ester-->2-Amino-4-bromophenol |
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