Cas No.: | 346640-08-2 |
Chemical Name: | CCF642 |
Synonyms: | CCF642;CCF-642;3-(4-Methoxyphenyl)-5-((5-nitrothiophen-2-yl)methylene)-2-thioxothiazolidin-4-one |
SMILES: | O=C1N(C2=CC=C(OC)C=C2)C(S/C1=C/C3=CC=C([N+]([O-])=O)S3)=S |
Formula: | C15H10N2O4S3 |
M.Wt: | 378.446 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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. |