CEP-33779
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.
CEP-33779是一种高度选择性和口服活性的Janus激酶2(JAK2)抑制剂。对JAK家族的其它成员进行评估时,CEP-33779显现出不同程度的选择性,从大于40倍的JAK1拮抗作用至大于800倍的TYK2拮抗作用。在细胞系统中,利用GeneBLAzer报告基因试验,CEP-33779显现出抑制irf-bla TF-1细胞中的JAK2的作用。它也能够降低与SLE进展相关的多个免疫参数,包括对狼疮性肾炎小鼠的保护和治疗。CEP-33779通过抑制IL-6/JAK2/STAT3信号以抑制结直肠肿瘤生长的能力表明,JAK2抑制剂在多种肿瘤类型中的潜在疗效,特别是那些具有强炎症成分的。
参考文献:
Kristine L Stump, Lily D Lu, Pawel Dobrzanski, Cynthia Serdikoff, Diane E Gingrich, Ben J Dugan, Thelma S Angeles, Mark S Albom, Mark A Ator, Bruce D Dorsey, Bruce A Ruggeri, Matthew M Seavey. A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Arthritis Research & Therapy 2011, 13:R68.
Lily D. Lu, Kristine L. Stump, Nate H. Wallace, Pawel Dobrzanski, Cynthia Serdikoff, Diane E. Gingrich, Benjamin J. Dugan, Thelma S. Angeles, Mark S. Albom, Jennifer L. Mason, Mark A. Ator, Bruce D. Dorsey, Bruce A. Ruggeri, Matthew M. Seavey. Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2. The Journal of Immunology October 1, 2011 vol. 187 no. 7 3840-3853.
Matthew M. Seavey, Lily D. Lu, Kristine L. Stump, Nate H. Wallace, William Hockeimer, Teresa M. O'Kane, Bruce A. Ruggeri, Pawel Dobrzanski. Therapeutic Efficacy of CEP-33779, a Novel Selective JAK2 Inhibitor, in a Mouse Model of Colitis-Induced Colorectal Cancer. Mol Cancer Ther April 2012 11; 984.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 462.57 |
Cas No. | 1257704-57-6 |
Formula | C24H26N6O2S |
Synonyms | CEP 33779,CEP33779 |
Solubility | ≥23.15 mg/mL in DMSO with gentle warming; insoluble in EtOH |
Chemical Name | N-[3-(4-methylpiperazin-1-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC1)C2=CC(=CC=C2)NC3=NN4C=CC=C(C4=N3)C5=CC=C(C=C5)S(=O)(=O)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。 |
描述 | CEP-33779是JAK2的选择性抑制剂,IC50值为1.8 nM。 | |||||
靶点 | JAK2 | |||||
IC50 | 1.8 nM |