NKP-1339

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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。

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 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℃, 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。