INK1117
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 5mg | ¥1081.00 | 10-15工作日发货 | |
| 10mg | ¥1636.00 | 10-15工作日发货 | |
| 25mg | ¥3490.00 | 10-15工作日发货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
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.
产品性质
| 物理外观 | A crystalline solid |
| CAS号 | 1268454-23-4 |
| 分子式 | C19H17N5O3 |
| 分子量 | 363.4 |
| 小分子别名 | Serabelisib |
| 化学名称 | [6-(2-amino-5-benzoxazolyl)imidazo[1,2-a]pyridin-3-yl]-4-morpholinyl-methanone |
| 溶解度 | ≤1mg/ml in DMSO;0.25mg/ml in dimethyl formamide |
| SMILES | Nc1nc(cc(cc2)-c(cc3)c[n]4c3ncc4C(N3CCOCC3)=O)c2[o]1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | Serabelisib(MLN1117)是一种选择性 p110α 抑制剂,IC50 为 15 nM。 |



沪公网安备 31011002003500