CCF642 |
| Catalog No.GC32893 |
CCF642는 IC50이 2.9μM인 강력한 PDI(단백질 이황화 이성화효소) 억제제입니다. CCF642는 세포 사멸을 유도하는 칼슘 방출을 동반하는 다발성 골수종 세포에서 급성 소포체(ER) 스트레스를 유발합니다. CCF642는 광범위한 항다발성 골수종 활성을 가지고 있습니다.
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.
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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