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CEP-1347
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CEP-1347图片
CAS NO:156177-65-0
规格:≥98%
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) C33H33N3O5S2
Formula 615.76
CAS No. 156177-65-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>10 mM
Water: <1mg/mL
Ethanol: <1mg/mL
Chemical NameMethyl (5S,6R,8R)-2,11-bis((ethylthio)methyl)-6-hydroxy-5-methyl-13-oxo-5,6,7,8,14,15-hexahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-6-carboxylate
SynonymsKT-7515; KT 7515; KT7515; CEP-1347; CEP 1347; CEP1347; 3,9-Bis((ethylthio)methyl)-K-252a; 3,9-Bis(etsm)-K-252a
实验参考方法
In Vitro

In vitro activity: In vitro, CEP-1347 efficiently induced differentiation and inhibited the self-renewal and tumor-initiating capacities of human cancer stem cells from glioblastoma as well as from pancreatic and ovarian cancers at clinically-relevant concentrations, without impairing the viability of normal fibroblasts and neural stem cells.


Kinase Assay: CEP-1347 (also known as KT7515), a derivative of the natural product K-252a found in broths of Narcodiopsis bacterium, is a novel and potent JNK inhibitor with IC50 of 30 nM on JNK1.


Cell Assay: Knockdown of survivin overexpressed in ovarian Chemoresistance of cancer stem cells (CSCs) resulted in increased sensitivity to paclitaxel. Treatment at clinically relevant concentrations with CEP-1347, a mixed lineage kinase inhibitor with a known safety profile in humans, reduced survivin expression in ovarian CSCs and sensitized them to paclitaxel.

In VivoIn vivo, a 10-day systemic administration of CEP-1347 at a dose that was less than 1/10 the mouse equivalent of the dose safely given to humans for 2 years was sufficient to effectively reduce tumor-initiating cancer stem cells within established tumors in mice. Furthermore, the same treatment protocol significantly extended the survival of mice receiving orthotopic implantation of glioma stem cells. Together, the findings suggest that CEP-1347 is a promising candidate for cancer stem cell-targeting therapy and that further clinical and preclinical studies are warranted to evaluate its efficacy in cancer treatment.
Animal modelMice with an orthotopic brain tumor model
Formulation & DosageMice (n = 6 for each group) implanted intracranially with GS-Y03 cells (1 × 104) underwent a daily intraperitoneal injection of the control vehicle or CEP-1347 (1.5 mg/kg/day) for 10 consecutive days, which started on the next day of intracranial implantation.
References Anticancer Res. 2018 Aug;38(8):4535-4542; Oncotarget. 2017 Oct 24;8(55):94872-94882.