CCF642 |
| カタログ番号GC32893 |
CCF642 は、IC50 が 2.9 μM の強力なプロテイン ジスルフィド イソメラーゼ (PDI) 阻害剤です。 CCF642 は、アポトーシス誘導カルシウム放出を伴う多発性骨髄腫細胞に急性小胞体 (ER) ストレスを引き起こします。 CCF642 には、幅広い抗多発性骨髄腫活性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 346640-08-2
Sample solution is provided at 25 µL, 10mM.
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CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.The IC50 is 2.9 μmol/L.In vitro: CCF642 inhibit PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. CCF642 causes acute ER stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release.In vivo: CCF642 displayed potent efficacy in an aggressive syngeneic mouse model of multiple myeloma and prolonged the lifespan of C57BL/KaLwRij mice engrafted with 5TGM1-luc myeloma, an effect comparable to the first-line multiple myeloma therapeutic bortezomib. CCF642 can be given intravenously without injection reactions in mice with 10 mg/kg.
[1]. Vatolin S et al. Novel Protein Disulfide Isomerase Inhibitor with Anticancer Activity in Multiple Myeloma. Cancer Res. 2016 Jun 1;76(11):3340-50.
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