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CEP-33779
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产品介绍
产品介绍
产品信息
抗原名称
JAK2,JAK3
商品描述
CEP-33779 is a novel, selective, and orally bioavailable inhibitor of JAK2 with an IC50 of 1.8±0.6 nM.
分子量
462.57
纯度
98%
可溶性
DMSO : 50 mg/mL (108.09 mM; Need ultrasonic)
In vitro(体外研究)
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(体内研究)
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.
背景
别名
CEP33779
分子式
C24H26N6O2S
CAS号
1257704-57-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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