CS-2765

生物活性靶点体外研究体内研究 CS-2765 试剂级价格

CS-2765

CAS号:197723-00-5
英文名:NKP-1339
中文名:CS-2765
CBNumber:CB62628194
分子式:C14H12Cl4N4NaRu
分子量:502.14365
MOL File:197723-00-5.mol

CS-2765化学性质

储存条件 :Store at -20°C
溶解度 :Ethanol: soluble
形态 :A solid
颜色 :Light brown to khaki

CS-2765性质、用途与生产工艺

生物活性 NKP-1339 (IT-139; KP-1339) 是针对实体癌开发的一流钌抗癌试剂，副作用小。NKP-1339 通过线粒体途径诱导 G2/M 细胞周期停滞，DNA 合成阻断 (DNA synthesis) 和诱导细胞凋亡 (apoptosis)。NKP-1339 具有很高的肿瘤靶向潜力，与血清蛋白 (serum proteins) 如白蛋白和转铁蛋白强烈结合，并在还原性肿瘤环境中激活。
靶点

Apoptosis

体外研究

NKP-1339 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC ₅₀ values of 45-200 μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC ₅₀ value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC ₅₀ values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively. NKP-1339 (0-150 μM; 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 (0-150 μM; 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:	0 μM, 50 μM, 100 μM, 150 μM and 200 μM
Incubation Time:	72 hours
Result:	Has anti-cancer activity in diverse malignant tumour cell types.

Apoptosis Analysis

Cell Line:	Hep3B cells
Concentration:	0 μM, 75 μM, 150 μM
Incubation Time:	72 hours
Result:	Promoted cell apoptosis as a concentration manner.

Western Blot Analysis

Cell Line:	Hep3B cells
Concentration:	0 μM, 75 μM, 150 μM
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; 30 mg/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:	30 mg/kg
Administration:	Intravenous injection
Result:	Had synergistic activity of KP1339 with sorafenib in vivo.