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CAS No.: 55661-38-6

Nimustine HCl/盐酸尼莫司汀 Catalog No. CSN21761

Synonyms: ACNU;Nidran HCl;Nimustine (hydrochloride)

Nimustine HCl is a nitrosourea alkylating agent with antineoplastic activity.

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技术信息

生物活性

描述Nimustine is a DNA alkylating and DNA cross-linking agent that induces DNA replication blocking lesions. It is commonly used in chemotherapy for glioblastomas. Nimustine at a concentration of 10µM and 30µM induced the frequency of homologous recombination in SPD8 cells by 7.2-fold and 13.9-fold, respectively, compared with untreated control cells^[2]. Treatment of glioma cell line LN-229 with 50µM nimustine for 48-144 hours induced apoptotic cell death in a time-dependent manner. Nimustine at 50µM also activated the MAPK signaling in LN-229 cells^[3]. Hyperbaric oxygen therapy has been shown to exert a sensitizing effect on nimustine therapy (3mg/kg; i.p.; once per week for 3 weeks) in mice inoculated with human glioma cells SU3^[4].
作用机制Nimustine is a synthesized, antitumor nitrosourea that can induce the formation of DNA alkali labile sites by causing damage or modification at positions corresponding to guanine moieties^[1].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02698280	Glioblastoma	Phase 2	Completed	-	China, Shanghai ... more >> Huashan hospital, Fudan University Shanghai, Shanghai, China, 200040 Collapse <<

参考文献

[1] Mineura K, Fushimi S, Itoh Y, Kowada M. DNA lability induced by nimustine and ramustine in rat glioma cells. J Neurol Neurosurg Psychiatry. 1988;51(11):1391-1394
[2] Kondo N, Takahashi A, Mori E, et al. FANCD1/BRCA2 plays predominant role in the repair of DNA damage induced by ACNU or TMZ. PLoS One. 2011;6(5):e19659
[3] Tomicic MT, Meise R, Aasland D, et al. Apoptosis induced by temozolomide and nimustine in glioblastoma cells is supported by JNK/c-Jun-mediated induction of the BH3-only protein BIM. Oncotarget. 2015;6(32):33755-33768
[4] Lu Z, Ma J, Liu B, et al. Hyperbaric oxygen therapy sensitizes nimustine treatment for glioma in mice. Cancer Med. 2016;5(11):3147-3155

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2347 mL
- 16.1734 mL
- 32.3468 mL
- 5 mM
- 0.6469 mL
- 3.2347 mL
- 6.4694 mL
- 10 mM
- 0.3235 mL
- 1.6173 mL
- 3.2347 mL

技术信息

CAS号

55661-38-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H14Cl2N6O2

运输

蓝冰

分子量

309.15

别名

ACNU;Nidran HCl;Nimustine (hydrochloride);NSC-D 245382;NSC-245,382

溶解度

DMSO	270.0 mg/mL (873.4 mM)
Water	75.0 mg/mL (242.6 mM)

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