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My CartCAS：1257704-57-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 1257704-57-6 |
| Name | CEP-33779 |
| Molecular Formula | C24H26N6O2S |
| Molecular Weight | 462.57 |
| Solubility | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD22683932 |
| SMILES | O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O |
| Target Point | JAK |
| Passage | JAK/STAT Signaling |
| Background | CEP-33779 is a novel, selective JAK2 inhibitor. |
| Biological Activity | 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。[1-3] |
| IC50 | JAK2:1.8nM;JAK3:150nM [1-3] |
| In Vitro | CEP-33779在无毒浓度下，对过量表达多药耐药细胞的P-糖蛋白过表达其抗癌底物敏感。 CEP-33779通过抑制P-糖蛋白转运功能的过度表达，显着增加细胞内积聚并减少阿霉素的外排[3]。 |
| In Vivo | CEP-33779在裸鼠中表现出有利的PK特征，静脉内半衰期为1小时，中度分布(Vd = 2.6L / kg)，并且可测量的口服暴露，估计的生物利用度为33％。它证明了CWR22异种移植模型的抗肿瘤功效;以30mg / kg bid口服给药14天导致5/10只动物的肿瘤停滞和部分消退[1]。 CEP-33779给药导致大多数动物肿瘤几乎完全萎缩;少数剩余的肿瘤结节小，血管化不良，并且有坏死的外观。 CEP-33779抑制肿瘤中NF-κB的激活[2]。 |
| Animal Experiment | 小鼠：携带CWR22异种移植物的裸鼠口服给予55mg / kg CEP-33779或载体(PEG400)。在给药后2，6和24小时，处死动物(3只/组)，切除肿瘤并制备血浆样品。使用补充有蛋白酶和磷酸酶抑制剂的基于Triton的提取缓冲液制备肿瘤提取物。在SDS-PAGE凝胶上分离等量的提取物，并使用特异性抗体通过蛋白质印迹分析STAT3磷酸化和表达[1]。 |
| Kinase Experiment | 测量杆状病毒表达的人JAK1，JAK2或JAK3的激酶活性。每个96孔Costar高结合板在TBS中在37℃下用100μL/孔的10μg/ mL中性抗生物素蛋白包被在37℃下2小时，然后在37°下用100μL/孔的1μg/ mL 15-mer肽底物包被C 1小时。激酶测定混合物(总体积=100μL/孔)由20mM HEPES(pH 7.2)，ATP(JAK1和JAK2为0.2μMATP，JAK3为0.1μMATP)，1mM MnCl 2，0.1％BSA和CEP组成将-33779(在DMSO中稀释，在测定中最终2.5％DMSO)加入测定板中。加入酶，使反应在室温下进行20分钟。通过添加100μL/孔稀释的Eu-N1标记的PY100抗体来进行磷酸化产物的检测。将样品在室温下孵育1小时，然后加入100μL增强溶液。将板搅拌10分钟，并测量所得溶液的荧光。确定IC50值[1]。 |
| Data Literature Source | [1]. Dugan BJ，et al. 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. [2]. Seavey MM，et al. Therapeutic efficacy of CEP-33779，a novel selective JAK2 inhibitor，in a mouse model of colitis-induced colorectal cancer. Mol Cancer Ther. 2012 Apr;11(4):984-93. [3]. Tang SJ，et al. CEP-33779 antagonizes ATP-binding cassette subfamily B member 1 mediated multidrug resistance by inhibiting its transport function. Biochem Pharmacol. 2014 Sep 15;91(2):144-56 |
| Unit | Bottle |
| Specification | 2mg 5mg |
CEP-33779是一个新颖的，选择性的JAK2抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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