CCF642

Research use only, not for human use.

CCF642 is a novel PDI-inhibiting compound with antimyeloma activity.

CCF-642 is a protein disulfide isomerase (PDI) inhibitor. CCF642 exhibited a submicromolar IC50 in 10 of 10 multiple myeloma cell lines. In vitro, CCF642 inhibited PDI reductase activity about 100-fold more potently than the structurally distinct established inhibitors PACMA 31 and LOC14. 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.

Western Blot Analysis Cell Line:MM1.S cells Concentration:3 μM Incubation Time:0.5, 1, 2, 4, 6 hours Result:Increased PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins.

Animal Model:C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc Dosage:10 mg/kg Administration:i.p.; three times a week; for 24 days Result:Significantly prolonged life of 5TGM1-luc–bearing mice and suppressed 5TGM1-luc growth as determined by life imaging.

CCF-642 | CCF 642 | CCF642

Angiogenesis

EGFR

protein disulfide isomerases

Cancer

——

346640-08-2

378.45

C15H10N2O4S3

>98% (HPLC)

DMSO : ≥ 30 mg/mL; 79.27 mM

S1C(=S)N(C(=O)/C/1=C\c1ccc(s1)[N+](=O)[O-])c1ccc(cc1)OC

3-(4-Methoxyphenyl)-5-[(5-nitro-2-thienyl)methylene]-2-thioxo-4-thiazolidinone

(-20℃)

With Ice Pack

≥ 2 years