Deltarasin
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.
KRAS癌基因产物被认为是抗癌药物开发的一个主要靶点。通过小分子方式干扰哺乳动物PDEδ与KRAS的结合,为通过改变致癌RAS在内膜上的定位从而抑制其信号传导提供了新的机会。Deltarasin是一种KRAS-PDEδ相互作用抑制剂,削弱致癌KRAS信号传导。
体外:一分钟内,5 mM的deltarasin完全抑制PDEδ-KRAS相互作用,并释放不溶物mCitrine-RHEB/KRAS6Q到内膜系统。这表明,deltarasin干扰细胞中KRAS与PDEδ的结合,从而抑制其溶解[1]。
体内:与注射赋形剂的对照组相比,deltarasin治疗的小鼠可观察到Panc-Tu-I肿瘤生长速度明显的剂量依赖性降低,其中用10 mg/kg BID deltarasin治疗的小鼠肿瘤生长几乎被完全阻断[1]。
临床试验:无临床数据可用。
参考文献:
[1] Zimmermann G, Papke B, Ismail S, Vartak N, Chandra A, Hoffmann M, Hahn SA, Triola G, Wittinghofer A, Bastiaens PI, Waldmann H. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013;497(7451):638-42.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 603.75 |
Cas No. | 1440898-61-2 |
Formula | C40H37N5O |
Solubility | Soluble in DMSO |
Chemical Name | (S)-1-benzyl-2-(4-(2-(2-phenyl-1H-benzo[d]imidazol-1-yl)-2-(piperidin-4-yl)ethoxy)phenyl)-1H-benzo[d]imidazole |
SDF | Download SDF |
Canonical SMILES | [H][C@@](C1CCNCC1)(N2C3=CC=CC=C3N=C2C4=CC=CC=C4)COC5=CC=C(C6=NC7=CC=CC=C7N6CC8=CC=CC=C8)C=C5 |
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。 |