Oncrasin 1
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Oncrasin 1是一种小分子抗肿瘤剂,IC50值为4.81 μM[1]。
Ras基因(K-Ras、N-Ras和H-Ras)激活突变在肿瘤发生和恶性表型的维持方面具有重要作用。突变使得Ras组成型处于与GTP结合的激活状态。在三个Ras基因中,K-Ras的突变是肿瘤中最频繁发生的,与放疗、化疗的耐受性及预后不良相关。因此,突变的K-Ras是抗癌治疗的重要靶标。Oncrasin 1是一种小分子化合物,通过合成致死筛选而发现,它通过诱导细胞凋亡,可有效杀死含K-Ras突变的肿瘤细胞,而非正常基因的细胞。此外,Oncrasin 1引起那些敏感细胞中PKCι的异常聚集[1]。
在磺酰罗丹明(SRB)实验中,Oncrasin 1以5 μg/ml的终浓度处理可杀死超过50%的细胞。Oncrasin 1对K-Ras突变具有高选择性,在T29Kt1(K-Ras突变)细胞中具有剂量依赖的细胞毒性,IC50值为4.81 μM。而对于T29Ht1(H-Ras突变)细胞和T29(野生型Ras)细胞,Oncrasin 1在浓度高达33 μM时仍未显示出细胞毒性。对于其它K-ras突变的肿瘤细胞,如A549、H2122和H460,Oncrasin 1均具有细胞毒性,IC50值均≤ 3 μM。据报道,诱导细胞凋亡是Oncrasin 1作用的主要机制[1]。
在注射H460细胞的小鼠中,Oncrasin 1以100 mg/kg的剂量给药后导致75.4%的显著肿瘤生长抑制。此外,Oncrasin 1治疗也延长了存活时间[1]。
参考文献:
[1] Guo W, Wu S, Liu J, et al. Identification of a small molecule with synthetic lethality for K-ras and protein kinase C iota. Cancer research, 2008, 68(18): 7403-7408.
Physical Appearance | Pale yellow solid |
Storage | Store at 4°C |
M.Wt | 269.73 |
Cas No. | 75629-57-1 |
Formula | C16H12CINO |
Solubility | Soluble in DMSO |
Chemical Name | 1-[(4-chlorophenyl)methyl]indole-3-carbaldehyde |
SDF | Download SDF |
Canonical SMILES | C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
化学结构
![Oncrasin 1](http://www.apexbt.com//media/diy/images/struct/A4454.png)