您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > NKP-1339
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
NKP-1339
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NKP-1339图片
CAS NO:197723-00-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
IT-139
KP-1339
产品介绍
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。
生物活性

NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solidcancerwith limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage ofDNA synthesis, and induction ofapoptosisvia the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds toserum proteinssuch as albumin and transferrin and activates in the reductive tumor milieu[1].

IC50& Target

Apoptosis[1]

体外研究
(In Vitro)

NKP-1339 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC50values of 45-200 μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC50value 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 IC50values 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[2].
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[2].
NKP-1339 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment[2].

Cell Viability Assay[2]

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[2]

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[2]

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
(In Vivo)

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[2].

Animal Model:Hep3B xenograft in Balb/c mice[2]
Dosage:30 mg/kg
Administration:Intravenous injection
Result:Had synergistic activity of KP1339 with sorafenib in vivo.
Clinical Trial
分子量

502.14

性状

Solid

Formula

C14H12Cl4N4NaRu

CAS 号

197723-00-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 59 mg/mL(117.50 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9915 mL9.9574 mL19.9148 mL
5 mM0.3983 mL1.9915 mL3.9830 mL
10 mM0.1991 mL0.9957 mL1.9915 mL
*

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
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。