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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1257704-57-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1221.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥500.0 |
| 规格： | 5 mg | 产品价格： | ￥1200.0 |
| 规格： | 10 mg | 产品价格： | ￥1800.0 |
| 规格： | 25 mg | 产品价格： | ￥3163.0 |
| 规格： | 50 mg | 产品价格： | ￥4500.0 |
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CEP-33779
CAS No. : 1257704-57-6
MCE 国际站：CEP-33779
产品活性：CEP-33779是一个新颖的，选择性，有口服活性的JAK2抑制剂，IC50值为1.8±0.6 nM。
研究领域：Epigenetics | Protein Tyrosine Kinase/RTK | JAK/STAT Signaling | Stem Cell/Wnt
作用靶点：JAK
In Vitro: CEP-33779, at nontoxic concentrations, significantly sensitizes overexpression of P-glycoprotein overexpressing multidrug resistance cells to its anticancer substrates. CEP-33779 significantly increases intracellular accumulation and decreases the efflux of doxorubicin by inhibiting the overexpression of P-glycoprotein transport function.
In Vivo: CEP-33779 exhibits a favorable PK profile in nude mice, an iv half-life of 1 h, moderate distribution (Vd=2.6 L/kg), and measurable oral exposure with an estimated bioavailability of 33%. It demonstrates antitumor efficacy in the CWR22 xenograft model; oral dosing for 14 days at 30 mg/kg bid results in tumor stasis and partial regressions in 5/10 animals. CEP-33779 administration results in an almost complete shrinkage of tumors in most animals; few remaining tumor nodules were small, poorly vascularized, and had a necrotic appearance. CEP-33779 suppressed activation of NF-κB in tumors.
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