NKP-1339(Synonyms: IT-139; KP-1339)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NKP-1339 (Synonyms: IT-139; KP-1339) 纯度: 98.14%

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。

NKP-1339(Synonyms: IT-139; KP-1339)

NKP-1339 Chemical Structure

CAS No. : 197723-00-5

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3866 In-stock
5 mg ￥3500 In-stock
10 mg ￥5000 In-stock
50 mg ￥15000 In-stock
100 mg ￥21000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

NKP-1339 相关产品

•相关化合物库:

  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Anti-Aging Compound Library
  • Anti-Lung Cancer Compound Library

生物活性

NKP-1339 (IT-139; KP-1339) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. NKP-1339 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. NKP-1339 has a high tumor targeting potential, strongly binds to serum proteins such 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 IC50 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 IC50 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 IC50 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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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

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 mg 5 mg 10 mg
1 mM 1.9915 mL 9.9574 mL 19.9148 mL
5 mM 0.3983 mL 1.9915 mL 3.9830 mL
10 mM 0.1991 mL 0.9957 mL 1.9915 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Robert Trondl, et al. NKP-1339, the first ruthenium-based anticancer drug on the edge to clinical application. Chemical Science. Chemical Science

    [2]. Heffeter P, et al. The ruthenium compound KP1339 potentiates the anticancer activity of sorafenib in vitro and in vivo. Eur J Cancer. 2013 Oct;49(15):3366-75.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务