PLX647
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.
PLX647是FMS和KIT激酶的有效特异性双重抑制剂,IC50值分别为28和16 nM[1].
麦克唐纳猫肉瘤病毒(v-fms)癌基因同源基因FMS,也称为CSF1R,是血小板衍生生长因子受体(PDGFR)家族的成员.巨噬细胞集落刺激因子(M-CSF或CSF-1)和白细胞介素34是两个已知的FMS配体.FMS在调节细胞存活\增殖和单核细胞/巨噬细胞谱系分化中发挥重要作用.干细胞因子(SCF)受体v-kit Hardy-Zuckerman 4猫肉瘤病毒致癌基因同源物(KIT)也属于PDGFR家族.在许多癌症中存在KIT的突变激活[1].
PLX647是FMS和KIT激酶的强效特异性双重抑制剂.PLX647的水溶性为14 μM.PLX647结合自抑制状态KIT激酶的近膜域,阻止活化环采用DFG-in构象.在表达活化蛋白激酶(BCR)-FMS和BCR-KIT的Ba/F3细胞中,PLX647抑制细胞增殖的IC50值分别为0.092和0.18 μM.此外,PLX647抑制破骨细胞分化,IC50值为0.17 μM[1].
在小鼠中,40 mg/kg的PLX647将LPS诱导的TNF-α和IL-6的释放分别减少85％和75％.在急性肾炎小鼠模型中,40 mg/kg的PLX647每天两次,将F4/80+巨噬细胞的水平减少77％[1].
参考文献：
[1]. Zhang C, Ibrahim PN, Zhang J, et al. Design and pharmacology of a highly specific dual FMS and KIT kinase inhibitor. Proc Natl Acad Sci U S A, 2013, 110(14): 5689-5694.
| Storage | Store at -20°C |
| M.Wt | 382.38 |
| Cas No. | 873786-09-5 |
| Formula | C21H17F3N4 |
| Solubility | insoluble in H2O; ≥1.63 mg/mL in EtOH with gentle warming and ultrasonic; ≥19.1 mg/mL in DMSO |
| Chemical Name | (E)-N-(5-((1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)pyridin-2(1H)-ylidene)-1-(4-(trifluoromethyl)phenyl)methanamine |
| SDF | Download SDF |
| Canonical SMILES | FC(F)(F)C1=CC=C(C/N=C2C=CC(CC3=CNC4=C3C=CC=N4)=CN\2)C=C1 |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
