K-Ras(G12C) inhibitor 9
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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.
靶点:K-Ras(G12C)
IC50:N/A
K-Ras(G12C) inhibitor 9是致癌K-ras(G12C)的变构抑制剂[1]。Ras蛋白属于GTP酶大家族,对于细胞外信号转导具有重要作用,包括增殖、分化和凋亡等不同的细胞应答。约30%的人类癌症中包含活化的Ras突变,使它们成为癌症最常见的遗传分子驱动剂[2]。因此,K-Ras信号在癌症中具有潜在的治疗优势。K-ras(G12C)存在于大约10-20%的Ras驱动的癌症中,并存在于大约50%的Ras突变的肺腺癌中[3]。
体外实验:K-Ras(G12C) inhibitor 9属于小分子,其不可逆地与GTP和GDP竞争结合致癌K-ras(G12C)突变体,阻断B-Raf和C-Raf与K-Ras(G12C)的关联。10 μM的K-Ras(G12C) inhibitor 9降低细胞活力,增加含有G12C突变的肺癌细胞系的凋亡,如H1792、Calu-1、H358和H23[1]。
体内:N/A
参考文献:
1. Ostrem JM, Peters U, Sos ML, Wells JA, Shokat KM. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013;503(7477):548-51.
2. Hunter JC, Gurbani D, Ficarro SB, Carrasco MA, Lim SM, Choi HG, et al. In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C. Proc Natl Acad Sci U S A. 2014;111(24):8895-900.
3. Lim SM, Westover KD, Ficarro SB, Harrison RA, Choi HG, Pacold ME, et al. Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor. Angew Chem Int Ed Engl. 2014;53(1):199-204.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 513.78 |
Cas No. | 1469337-91-4 |
Formula | C16H21ClIN3O4S |
Solubility | Soluble in DMSO |
Chemical Name | N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide |
SDF | Download SDF |
Canonical SMILES | C=CS(NC1CCN(C(CNC2=C(OC)C=C(Cl)C(I)=C2)=O)CC1)(=O)=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。 |