Neocarzinostatin

Neocarzinostatin用途

Neocarzinostatin 是一种有效的 DNA 损伤的、抗肿瘤抗生素,可识别双链 DNA 膨胀并诱导DNA双链断裂 (DSBs)。Neocarzinostatin 诱导细胞凋亡 (apoptosis)。Neocarzinostatin 具有用于 EpCAM 阳性肿瘤的潜力。

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Neocarzinostatin名称

[ CAS 号 ]:
9014-02-2

[ 英文名 ]:
Neocarzinostatin

Neocarzinostatin生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

[体外研究]

EpCAM适体结合的新胡萝卜素(NCS)对EpCAM阳性细胞具有特异性。共轭物对癌细胞的作用令人印象深刻,因为共轭物阻止细胞周期,促进细胞凋亡和坏死。高水平的PARP表达证实了结合处理后DNA的断裂。与EpCAM结合的NCS可靶向于癌细胞而不靶向于正常细胞[3]。Neocarzinostatin(72小时)对C6细胞和U87MG细胞的IC50值分别为493.64nm和462.96nm[4]。在不同组织来源的人肿瘤细胞系中,对新卡星他汀的敏感性与Bcl-2和caspase-3相对含量的乘积成正比[5]。

[参考文献]

[1]. Athyala PK, et al. Probing the biophysical interaction between Neocarzinostatin toxin and EpCAM RNA aptamer. Biochem Biophys Res Commun. 2016 Jan 8;469(2):257-62.

[2]. Allen Taylor, et al. Ubiquitination capabilities in response to neocarzinostatin and H2O2 stress in cell lines from patients with ataxia-telangiectasia. Oncogene (2002) 21, 4363- 4373.

[3]. Athyala PK, et al. Neocarzinostatin, Aptamer Conjugates for Targeting EpCAM-positive Tumor Cells. Anticancer Res. 2017 Jul;37(7):3615-3629.

[4]. Tianqin G, et al. Synergistic Anti-glioma Effects in Vitro and in Vivo of Enediyne Antibiotic Neocarzinostatin and Paclitaxel via Enhanced Growth Delay and Apoptosis-Induction. Biol Pharm Bull. 2016 Oct 1;39(10):1623-1630.

[5]. Rogers D, et al. Molecular predictors of human nervous system cancer responsiveness to enediyne chemotherapy.

Neocarzinostatin物理化学性质

[ 密度 ]:
1.52g/cm3

[ 沸点 ]:
900.5ºC at 760 mmHg

[ 分子式 ]:
C₃₅H₃₅NO₁₂

[ 分子量 ]:
661.65200

[ 闪点 ]:
498.4ºC

[ 精确质量 ]:
661.21600

[ PSA ]:
174.77000

[ LogP ]:
1.85820

[ 折射率 ]:
1.688

Neocarzinostatin安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;half-mask respirator (US);multi-purpose combination respirator cartridge (US)

[ 危险品运输编码 ]:
NONH for all modes of transport

Neocarzinostatin文献

Neocarzinostatin-chromophore: a potent inhibitor of casein kinase II in vitro. Tanoue, S., et al.

Antibiotics 51 , 95-98, (1998)

The enediyne antibiotics.

J. Med. Chem. 39 , 2103-2117, (1996)

Reinvestigation of the proteolytic activity of neocarzinostatin.

J. Bacteriol. 182 , 1812-1818, (2000)

Neocarzinostatin (NCS) is the most studied member of a family of chromoproteins secreted by a range of actinomycetes species. It has been proposed that in addition to their antitumoral activity relate...

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