| CAS NO: | 1268454-23-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 363.4 |
| Cas No. | 1268454-23-4 |
| Formula | C19H17N5O3 |
| Synonyms | MLN1117,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 |
| Canonical SMILES | NC1=NC2=CC(C(C=C3)=CN4C3=NC=C4C(N5CCOCC5)=O)=CC=C2O1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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