CCF642CAS号： 346640-08-2分子式： C15H10N2O4S3分子量： 378.45描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
CCF642 is a novel PDI-inhibiting compound with antimyeloma activity. |
| 纯度 |
＞98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
CCF 642；CCF-642；AC1LYELL
|
| 外观 |
Powder
|
| 可溶性/溶解性 |
DMSO ：15 mg/mL (39.64 mM)
|
| 生物活性 | |
| 靶点 |
protein disulfide isomerases
|
| In vitro(体外研究) |
In vitro, CCF642 inhibits PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. Computational modeling suggests a novel covalent binding mode in active-site CGHCK motifs. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release.
|
| In vivo(体内研究) |
CCF642 displays potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolongs the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib.
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| 参考文献 | |
| 参考文献 |
[1] Vatolin S, et al. Cancer Res. 2016, 76(11):3340-50. |
分子结构图
