Peficitinb (ASP015K, JNJ-54781532)
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.
Peficitinib(ASP015K)是一种口服Janus激酶(JAK)抑制剂。它能抑制JAK1、JAK2、JAK3和TYK2的酶活性,IC50值为3.9、5.0、0.71和4.8 nmol/L。对JAK3的抑制具有适度选择性[1]。
非受体蛋白酪氨酸激酶JAK家族包括JAK1、JAK2、JAK3和酪氨酸激酶2(TYK2)。 JAK1、JAK2、JAK3和TYK2对造血细胞和免疫细胞至关重要[1]。
促红细胞生成素调节造血,即血细胞生成[2]。ASP015K抑制由IL-2诱导的人T细胞的增殖,并且这种效果比抑制EPO诱导的人红白血病细胞增殖的影响更大。在人全血中,ASP015K能浓度依赖性地抑制STAT5磷酸化(pSTAT5)[3]。
在健康志愿者中, ASP015K剂量依赖性的抑制了STAT5-P。剂量为60、120、200或300 mg的 ASP015K 分别抑制84%、85%、92%和93%的STAT5-P。血浆ASP015K抑制STAT5-P,EC50值为48 ng/mL,形状因子(γ)约为1.2, Emax接近100%。多浓度ASP015K处理2 h后的第1、7和14天,出现STAT5-P抑制的中位数百分比的峰值[4]。
参考文献:
[1]. Takeuchi T, Tanaka Y, Iwasaki M, et al. Efficacy and safety of the oral Janus kinase inhibitor peficitinib (ASP015K) monotherapy in patients with moderate to severe rheumatoid arthritis in Japan: a 12-week, randomised, double-blind, placebo-controlled phase IIb study. Annals of the rheumatic diseases, 2015: annrheumdis-2015-208279.
[2]. Digicaylioglu M, Lipton SA. Erythropoietin-mediated neuroprotection involves cross-talk between Jak2 and NF-κB signalling cascades. Nature, 2001, 412(6847): 641-647.
[3]. Yamazaki S, Morio H, Inami M, et al. THU0101 ASP015K: A Novel Jak Inhibitor Demonstrated Potent Efficacy in Adjuvant-Induced Arthritis Model in Rats. Annals of the Rheumatic Diseases, 2013, 72(Suppl 3): A197-A197.
[4]. Zhu T, Valluri U, Lewand M, et al. THU0256 Pharmacodynamics of ASP015K, A Novel Janus Kinase Inhibitor, in Healthy Volunteers. Annals of the Rheumatic Diseases, 2013, 72(Suppl 3): A252-A252.
Storage | Store at -20°C |
M.Wt | 326.39 |
Cas No. | 944118-01-8 |
Formula | C18H22N4O2 |
Solubility | Soluble in DMSO |
Chemical Name | 4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-7H-pyrrolo[2,3-b]pyridine-5-carbimidic acid |
SDF | Download SDF |
Canonical SMILES | N=C(O)C1=CNC2=NC=CC2=C1N[C@]3([H])[C@@](C4)([H])C[C@@]5([H])C[C@]3([H])C[C@]4(O)C5 |
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。 |