Oncrasin-1

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Oncrasin-1  纯度: 99.79%

Oncrasin-1是高效的抗癌抑制剂,能低浓度下杀死各种K-Ras突变型人肺癌细胞。

Oncrasin-1

Oncrasin-1 Chemical Structure

CAS No. : 75629-57-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1188 In-stock
10 mg ¥1080 In-stock
50 mg ¥4760 In-stock
100 mg   询价  
200 mg   询价  

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生物活性

Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. IC50 value: 1.0 μM(A549, K-ras 12H and p53 Wt) [1] Target: human lung cancer cells with K-Ras mutation; K-Ras/PKCiota pathway inhibitor in vitro: effectively kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. The cytotoxic effects correlated with apoptosis inductionas was evidenced by increase of apoptotic cells and activation of caspase-3 and caspase-8 upon the treatment of oncrasin-1 in sensitive cells. Treatment with oncrasin-1 also led to abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells. Furthermore, oncrasin-1 induced apoptosis was blocked by siRNA of K-Ras or PKCι suggesting that oncrasin-1 is targeted to a novel K-Ras/PKCι pathway [1]. oncrasin-1 treatment led to coaggregation of PKCiota and splicing factors into megaspliceosomes but had no obvious effects on the DNA repair molecule Rad51. Moreover, oncrasin-1 treatment suppressed the phosphorylation of the largest subunit of RNA polymerase II and the expression of intronless reporter genes in sensitive cells but not in resistant cells [2]. in vivo: The in vivo administration of oncrasin-1 suppressed the growth of K-ras mutant human lung tumor xenografts by >70% and prolonged the survival of nude mice bearing these tumors, without causing detectable toxicity [1].

分子量

269.73

Formula

C16H12ClNO

CAS 号

75629-57-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 43 mg/mL (159.42 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 3.7074 mL 18.5371 mL 37.0741 mL
5 mM 0.7415 mL 3.7074 mL 7.4148 mL
10 mM 0.3707 mL 1.8537 mL 3.7074 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。-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]. Guo W, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer Res. 2008 Sep 15;68(18):7403-8.

    [2]. Guo W, et al. Interruption of RNA processing machinery by a small compound, 1-[(4-chlorophenyl)methyl]-1H-indole-3-carboxaldehyde (oncrasin-1). Mol Cancer Ther. 2009 Feb;8(2):441-8.

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