计算溶液所需的质量、体积或浓度。
为什么选择此级别
提供 ≥98% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis , and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.
In Vitro
BOLD-100 (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. BOLD-100 (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. BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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 AnalysisCell Line: Hep3B cells Concentration: 0 μM, 75 μM, 150 μM Incubation Time: 72 hours Result: Promoted cell apoptosis as a concentration manner. Western Blot AnalysisCell 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.
In Vivo
BOLD-100 (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 BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Hep3B xenograft in Balb/c miceDosage: 30 mg/kg Administration: Intravenous injection Result: Had synergistic activity of KP1339 with sorafenib in vivo.
Form:Solid
规格
规格或纯度
≥98%
英文名称
BOLD-100
生化机理
BOLD-100（NKP-1339；IT-139）是第一种正在开发中的钌基抗癌剂，可用于治疗实体瘤，且副作用有限。BOLD-100 可诱导 G2/M 细胞周期停滞、DNA 合成受阻，并通过有丝分裂诱导细胞凋亡。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥98%
名称和识别符
分子类型
小分子
分子量
502.14
技术文档
高级数据
化学和物理性质
溶解性
DMSO : ≥ 59 mg/mL (117.50 mM)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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