NKP-1339 ≥95%
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| 包装规格: | 1mg 5mg 10mg in glass bottle |
| 溶解性: | 溶于DMSO(≥ 59 mg/mL) |
| 产品描述: | 基本信息 产品编号:N10495 产品名称:NKP-1339 CAS: 197723-00-5 储存条件 粉末 -20℃ 四年 分子式: C14H12Cl4N4NaRu 溶于液体 -80℃ 六个月 分子量 502.14 -20℃ 一个月 化学名: Solubility (25°C) 体外 DMSO ≥59mg/mL (117.50mM) Ethanol Water 体内 现配现用 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 1.9915mL 9.9574mL 19.9148mL 5mM 0.3983mL 1.9915mL 3.9830mL 10mM 0.1991mL 0.9957mL 1.9915mL 生物活性 产品描述 一种钌基抗癌化合物。 靶点/IC50 Apoptosis 体外研究 NKP-1339 (0-200μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC50 values of 45-200μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC50 value of 186.3μM, 165.4μM, 124.4μM, and 69.4μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC50 values of 178μM, 111μM, and 143μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL8, SW480 and HCT116 cells, respectively NKP-1339 (0-150μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either. NKP-1339 (0-150μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment. Cell Viability Assay Cell Line: Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines Concentration: 0μM, 50μM, 100μM, 150μM and 200μM Incubation Time: 72 hours Result: Has anti-cancer activity in diverse malignant tumour cell types. Apoptosis Analysis Cell Line: Hep3B cells Concentration: 0μM, 75μM, 150μM Incubation Time: 72 hours Result: Promoted cell apoptosis as a concentration manner. Western Blot Analysis Cell Line: Hep3B cells Concentration: 0μM, 75μM, 150μM Incubation Time: 72 hours Result: Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment. 体内研究 NKP-1339 (intravenous injection; 30mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the NKP-1339 treatment alone in Hep3B xenografts grown in Balb/c SCID mice. Animal Model: Hep3B xenograft in Balb/c mice Dosage: 30mg/kg Administration: Intravenous injection Result: Had synergistic activity of KP1339 with sorafenib in vivo. |
| 保存条件: | -20℃ |
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