Decernotinib(VX-509)
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.
Decernotinib(VX-509)是一种新型的\有效的以及选择性的JAK3抑制剂,其Ki值为2 nM[1].
Janus激酶家族包括4个成员:JAK1\JAK2\JAK3和TYK2.Janus激酶3(JAK3)主要表达于淋巴细胞,而淋巴细胞在与许多疾病(包括类风湿性关节炎(RA))相关的免疫应答中起重要作用[1].
Decernotinib(VX-509)是一种新型的\有效的以及口服可用的JAK3抑制剂,用于治疗自身免疫性疾病.VX-509抑制JAK1\JAK2\JAK3和TYK2,其Ki值分别为11 nM\13 nM\2 nM和11 nM.在HT-2或TF-1细胞中,使用IL-2或GM-CSF刺激后,VX-509抑制JAK3/1或JAK2介导的STAT5磷酸化,其IC50值分别为99 nM和2600 nM[1].
在大鼠宿主抗移植物(HvG)模型中,相对于Cyclosporin A(CsA),VX-509(50 mg/kg,每日2次;100 mg/kg,每日1次)呈剂量依赖性地显著抑制66%以及94%的腘窝淋巴结(PLN)增生.VX-509也显著下调CD25表达.上述结果表明,VX-509具有显著的剂量依赖性免疫抑制活性,有效地抑制T细胞活化[1].在胶原诱导的大鼠关节炎模型中,VX-509呈剂量依赖性地减少踝关节肿胀以及爪重,并改善爪组织病理学得分.在Oxazolone诱导的小鼠迟发型超敏反应模型中,VX-509减少T细胞介导的皮肤炎性反应[2].
参考文献：
[1]. Farmer LJ, Ledeboer MW, Hoock T, et al. Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases. J Med Chem, 2015, 58(18): 7195-7216.
[2]. Mahajan S, Hogan JK, Shlyakhter D, et al. VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease. J Pharmacol Exp Ther, 2015, 353(2): 405-414.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 392.38 |
| Cas No. | 944842-54-0 |
| Formula | C18H19F3N6O |
| Solubility | insoluble in H2O; ≥16.95 mg/mL in DMSO; ≥2.92 mg/mL in EtOH with ultrasonic |
| Chemical Name | (R,Z)-2-((2-(1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)-2-methyl-N-(2,2,2-trifluoroethyl)butanimidic acid |
| SDF | Download SDF |
| Canonical SMILES | CC[C@](/C(O)=N/CC(F)(F)F)(NC1=NC(C2=CNC3=C2C=CC=N3)=NC=C1)C |
| 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
