JNJ-38877605
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.
JNJ-38877605是c-Met催化活性的ATP竞争性小分子抑制剂。
研究表明，c-Met信号参与几种癌症的增殖和扩散过程，加强了对其在疾病中作用的理解，激发了将c-Met和HGF 作为抗癌药物发展的主要靶标的兴趣。
体外实验：与大约250种酪氨酸和丝氨酸-苏氨酸激酶相比，JNJ-38877605对c-Met有大约600倍的选择性，有效抑制体外HGF刺激的和组成型激活的c-Met磷酸化[1]。
在体实验：在所检测的物种中，JNJ-38877605具有约100％的口服生物利用度。此外，在肿瘤异种移植模型中，单剂量JNJ-38877605可以抑制 Met磷酸化长达16个小时。不同口服给药方案中，Met磷酸化的抑制与剂量依赖性的肿瘤生长抑制相关[2]。
临床试验：在晚期或难治性实体瘤患者中进行了JNJ-38877605的安全性和剂量研究。
参考文献：
[1] PereraT, L avrijssenT, Janssens B, et al. JNJ-38877605: a selective Met kinase inhibitor inducing regression of Met-driven tumor models. Presented at the 99th AACR Annual Meeting; 2008 Apr 12 -16;
| Storage | Store at -20°C |
| M.Wt | 377.35 |
| Cas No. | 943540-75-8 |
| Formula | C19H13F2N7 |
| Solubility | insoluble in H2O; ≥18.85 mg/mL in DMSO; ≥3.25 mg/mL in EtOH with ultrasonic |
| Chemical Name | 6-[difluoro-[6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl]quinoline |
| SDF | Download SDF |
| Canonical SMILES | CN1C=C(C=N1)C2=NN3C(=NN=C3C(C4=CC5=C(C=C4)N=CC=C5)(F)F)C=C2 |
| 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。 |
| Description | JNJ-38877605是c-Met的ATP竞争性抑制剂，IC50值为4 nM。 | |||||
| 靶点 | c-Met | |||||
| IC50 | 4 nM | |||||
质量控制和MSDS
- 批次:
化学结构
