FRAX1036
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.
FRAX1036是一种p21活化激酶I(PAK1)抑制剂。
乳腺癌是一种临床和分子的异质性疾病,大量的乳腺肿瘤的遗传和表观遗传学研究揭示了新的假定驱动基因,如p21活化激酶(PAK)1。作为包括Rac1和Cdc42在内的小GTP结合蛋白下游的一种丝氨酸/苏氨酸激酶,PAK1是生长因子信号网络的关键组分,其细胞功能对肿瘤发生至关重要。
体外:先前的研究表明,docetaxel与FRAX1036或PAK1小干扰RNA寡核苷酸给药能够显著改变对细胞骨架相关蛋白的信号传导,例如stathmin,并且还能够诱导微管解体和细胞凋亡。此外,活细胞成像数据显示,docetaxel介导的有丝分裂阻滞持续时间可以通过FRAX1036治疗显著减少,这与细胞凋亡的动力学增加相关[1]。
体内:在先前的动物研究中,载有KT21移植物的未处理小鼠表现出心室侵袭,而Ben-Men在注射部位生长。功效研究结果发现,与载体对照相比,用Frax1036治疗可以导致肿瘤生长减缓,体重指数(BMI)信号减少37%[2]。
临床试验:到目前为止,FRAX1036仍处于临床前研究阶段。
参考文献:
[1] Ong CC et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res.2015 Apr 23;17:59.
[2] Chow HY et al. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget.2015 Feb 10;6(4):1981-94.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 518.05 |
Cas No. | 1432908-05-8 |
Formula | C28H32ClN7O |
Solubility | Soluble in DMSO |
Chemical Name | 6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one |
SDF | Download SDF |
Canonical SMILES | O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC |
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。 |