| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| C409131-1ml |
1ml |
现货  |
|
| 英文别名 | [1,2,4]Triazolo[1,5-a]pyridin-2-amine, N-[3-(4-methyl-1-piperazinyl)phenyl]-8-[4-(methylsulfonyl)phenyl]- |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | CEP-33779 |
| 生化机理 | CEP33779 是一种选择性 JAK2 抑制剂，其 IC50 值为 1.8 nM，与 JAK1 和 TYK2 相比分别提高了 40 倍和 800 倍以上。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | Janus 激酶 2 抑制剂;Janus 激酶 3 抑制剂 |
| 产品介绍 |
CEP-33779是一种选择性JAK2抑制剂，IC50为1.8 nM，比作用于JAK1和TYK2选择性高40多倍和800多倍。 Information CEP33779 is a selectiveJAK2inhibitor withIC50of 1.8 nM, >40- and >800-fold versus JAK1 and TYK2. CEP33779(< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5(pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells. In vivo CEP33779 orally administrated with 55 mg/kg inhibits phosphorylation of STAT5 in HEL92 tumor extracts from HEL92 xenograft mice. CEP33779 orally administered twice daily at dose of 55 mg/kg reduces mean paw edema and clinical scores in mice with collagen-antibody induced arthritis (CAIA) or collagen-induced arthritis (CIA). CEP33779 orally administered twice daily at dose of 55 mg/kg totally inhibits paw phospho-STAT3 expression in CAIA or CIA mice, associated with decreased cytokines including IL-12, IFNγ, IL-2, IL-1β, TNFα and GM-CSF. CEP33779 results in reduced bone degradation, reduced tissue destruction, and reduced osteoarthritis in dose-dependent manner in CAIA or CIA mice. CEP33779 orally administrated at 100 mg/kg extends survival and reduces splenomegaly/lymphomegaly in MRL/lpr systemic lupus erythematosus mice, thus protect mice from developing glomerulonephritis. CEP33779 orally administrated at 100 mg/kg decreases several SLE-associated proinflammatory cytokines and reduces levels of a bone resorption biomarker associated with increased osteoclast activity in MRL/lpr systemic lupus erythematosus mice. CEP33779 orally administered twice daily at dose of 55 mg/kg induces regression of established colorectal tumors, reduces angiogenesis, and reduces proliferation of tumor cells in a mouse model of colitis-induced colorectal cancer. Tumor regression correlated with inhibition of STAT3 and NF-κB (RelA/p65) activation, and decreased the expression of proinflammatory, tumor-promoting cytokines interleukin (IL)-6 and IL-1β. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| IC50 | JAK2, IC50: 1.8 nM |
|---|---|
| ALogP | 3.86 |
| hba_count | 4 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
| Canonical SMILES | CN1CCN(CC1)C2=CC=CC(=C2)NC3=N[N]4C=CC=C(C5=CC=C(C=C5)[S](C)(=O)=O)C4=N3 |
|---|---|
| 分子量 | 462.57 |
| Reaxy-Rn | 20921741 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20921741&ln= |
| 溶解性 | Solubility (25°C) In vitro |
|---|---|
| DMSO(mg / mL) Max Solubility | 36 |
| DMSO(mM) Max Solubility | 77.83 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 20921741 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=20921741&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
首页
400-620-6333
