Deltarasin hydrochloride
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.
Deltarasin hydrochloride是一种选择性的KRAS-PDEδ相互作用抑制剂,IC50值为41±12 nM 1]。
KRAS(V-Ki-ras2 Kirsten大鼠肉瘤病毒原癌基因同源物)是一种蛋白,作为分子开/关,其突变在许多癌症的的发展中是重要步骤。PDEδ(异戊烯基结合蛋白)控制K-Ras的空间组织,增强Ras在胞质溶胶中的扩散。小分子对Ras-PDEδ相互作用的抑制损害Ras的定位和信号,成为一种临床上治疗癌症的有前途的策略[1,2]。
Deltarasin hydrochloride是一种有效的KRAS-PDEδ相互作用抑制剂。在人胰腺导管腺癌细胞中,deltarasin hydrochloride通过与PDEδ结合,抑制KRAS-PDEδ相互作用,从而抑制致癌RAS信号,抑制细胞增殖,Kd值为41 nM[1]。
在Panc-Tu-I异种移植裸鼠模型中,deltarasin hydrochloride(10,15 mg/kg)在治疗9天后以剂量依赖的方式损害细胞生长,减少肿瘤体积[1]。
参考文献:
[1]. Zimmermann, G., et al., Small molecule inhibition of the KRAS-PDEdelta interaction impairs oncogenic KRAS signalling. Nature, 2013. 497(7451): p. 638-42.
[2]. The KRAS-PDEdelta interaction is a therapeutic target. Cancer Discov, 2013. 3(7): p. Of20.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 640.22 |
Cas No. | 1440898-82-7 |
Formula | C40H38ClN5O |
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 hydrochloride |
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.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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