K-Ras(G12C) inhibitor 12
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
K-Ras(G12C) inhibitor 12是K-Ras(G12C)的别构抑制剂[1].
K-Ras是一种GTPase,在多个信号转导途径中扮演重要角色.多种癌症中出现K-Ras突变.
K-Ras(G12C) inhibitor 12是K-Ras(G12C)的别构抑制剂.K-Ras(G12C)具有对GTP的轻微偏好.然而,K-Ras(G12C) inhibitor 12可显著降低对GTP的亲和性,引发K-Ras(G12C)修饰.并且,K-Ras(G12C) inhibitor 12可抑制SOS催化的核苷酸交换.在H1792和H358 K-Ras(G12C)突变肺癌细胞系中,K-Ras(G12C) inhibitor 12可减少C-Raf和B-Raf与Ras的关联.在包含G12C突变的H1792\H358\H23和Calu-1细胞系中,K-Ras(G12C) inhibitor 12可降低存活并可诱发细胞凋亡.K-Ras(G12C) inhibitor 12在H1792细胞中的EC50值为0.32 M.并且,H1792细胞具有低水平的K-Ras GTP,这与K-Ras(G12C) inhibitor 12对K-Ras GDP的偏好相一致[1].
参考文献：
[1]. Ostrem JM1, Peters U, Sos ML, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature, 2013, 503(7477): 548-551.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 449.67 |
| Cas No. | 1469337-95-8 |
| Formula | C15H17ClIN3O3 |
| Solubility | ≥8.98 mg/mL in DMSO with gentle warming |
| Chemical Name | 1-[4-[2-(4-chloro-2-hydroxy-5-iodoanilino)acetyl]piperazin-1-yl]prop-2-en-1-one |
| SDF | Download SDF |
| Canonical SMILES | C=CC(=O)N1CCN(CC1)C(=O)CNC2=CC(=C(C=C2O)Cl)I |
| 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。 |
| 细胞实验[1]： | |
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细胞系 |
肺癌细胞系H23, H358 和 H1792 |
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溶解方法 |
在DMSO中的溶解度有限。为了获得更高的浓度，可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
|
反应条件 |
72 h，10 μM |
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应用 |
K-Ras(G12C) inhibitor 12是一种高效的Ras抑制剂，在H1792细胞中的EC50是0.32 μM。它选择性地不可逆结合到K-Ras的G12C致癌突变体上，却不影响野生型Ras的活性。和没有突变的细胞比起来，用K-Ras(G12C) inhibitor 12处理后的K-Ras(G12C)突变细胞活力下降，凋亡增加。 |
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References: [1]. Ostrem J M, Peters U, Sos M L, et al. K-Ras (G12C) inhibitors allosterically control GTP affinity and effector interactions[J]. Nature, 2013, 503(7477): 548-551. | |
化学结构
相关生物数据
