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CAS No.: 1257704-57-6

CEP-33779 Catalog No. CSN15836

Synonyms: CEP-33779

CEP-33779 is a highly selective JAK2 inhibitor with IC50 value of 1.8 nM, with much less potency against JAK1 and TYK2 with >40- and >800-fold IC50 values.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 JAK2

IC50:1.8nM
描述The JAK/STAT pathway forms a critical node affecting multiple signaling pathways in both the innate and adaptive immune responses. Janus kinase 2 (JAK2) belongs to the non-receptor tyrosine kinase family. JAK2 is widely distributed in the cytoplasm of a variety of somatic cells, involved in cell-cycle regulation, apoptosis, mitotic chromosome recombination, genetic instability, and heterochromatin changes, and other biological processes. CEP-33779 is a highly selective, small-molecule inhibitor of JAK2 with an IC₅₀ of 1.8 nMDugan BJ, Gingrich DE, Mesaros EF, Milkiewicz KL, Curry MA, Zulli AL, Dobrzanski P, Serdikoff C, Jan M, Angeles TS, Albom MS, Mason JL, Aimone LD, Meyer SL, Huang Z, Wells-Knecht KJ, Ator MA, Ruggeri BA, Dorsey BD. A selective, orally bioavailable 1,2,4-triazolo[1,5-a]pyridine-based inhibitor of Janus kinase 2 for use in anticancer therapy: discovery of CEP-33779. J Med Chem. 2012 Jun 14;55(11):5243-54. doi: 10.1021/jm300248q. Epub 2012 May 18. PMID: 22594690.}https://pubmed.ncbi.nlm.nih.gov/22594690/. Administration of CEP-33779 in a therapeutic mode resulted in a reduction in colorectal tumor mass, decreased levels of proinflammatory cytokines, and inhibition of STAT3 and NF-κB activation. In addition, it caused histologic reductions in cancer grades, and a negative impact on the tumor microenvironment including reduced tumor cell proliferation and angiogenesis upon JAK2 inhibition. With advanced development, CEP-33779 can deplet the autoreactive plasma cells, treat lupus nephritis in mice, ablate disease in two different mouse models of rheumatoid arthritis and administration of CEP-33779 results in significant inhibition of tumor growth in an AOM/DSS-induced model of colorectal cancer^[3]. In a vitro study, KBV20C cells were then stimulated for 72h with CEP-33779 ranging from 5-10 μM. The result showed that JAK2 inhibitor CEP-33779 increased sensitization of KBV20C cells to VIC-induced mitotic-arrest^[4]. In a vivo study, using a mouse model of colitis-induced colorectal cancer, JAK2 inhibitor, CEP-33779 induced regression of established colorectal tumors, reduced angiogenesis, and reduced proliferation of tumor cells with an increasing doses of 10 mg/kg, 30 mg/kg, and 55 mg/kg^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
TF-1 cells	-	Function assay	1 h	Inhibition of JAK2 in human TF-1 cells using GM-CSF pretreated for 1 hr prior to GM-CSF addition measured after 5 hrs by FRET based GeneBLAzer assay, IC50=0.061 μM	22594690

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1618 mL
- 10.8092 mL
- 21.6185 mL
- 5 mM
- 0.4324 mL
- 2.1618 mL
- 4.3237 mL
- 10 mM
- 0.2162 mL
- 1.0809 mL
- 2.1618 mL

技术信息

CAS号

1257704-57-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26N6O2S

运输

蓝冰

分子量

462.57

别名

CEP-33779

溶解度

DMSO	36.0 mg/mL (77.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

1% DMSO+30% PEG 300+1% Tween 80+water

30 mg/mL

suspension

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