CCF642 |
| Catalog No.GC32893 |
CCF642 es un potente inhibidor de las proteÍnas disulfuro isomerasas (PDI) con una IC50 de 2,9 μM. CCF642 causa estrés agudo en el retÍculo endoplÁsmico (RE) en células de mieloma mÚltiple acompaÑado de liberaciÓn de calcio que induce la apoptosis. CCF642 tiene una amplia actividad contra el mieloma mÚltiple.
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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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