CAS NO: | 197723-00-5 |
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 |
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]
Apoptosis Analysis[2]
Western Blot Analysis[2]
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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].
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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
* 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。 |