| CAS NO: | 156177-65-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 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 Name | Methyl (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 |
| Synonyms | KT-7515; KT 7515; KT7515; CEP-1347; CEP 1347; CEP1347; 3,9-Bis((ethylthio)methyl)-K-252a; 3,9-Bis(etsm)-K-252a |
| 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 Vivo | In 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 model | Mice with an orthotopic brain tumor model |
| Formulation & Dosage | Mice (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. |
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