CCF-642


Catalog No. size PriceQuantity
M7086-2 2mg solid $88
M7086-10 10mg solid $360

Description

Cas:346640-08-2

Product Information

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.

 

Chemical Formula: C15H10N2O4S3

 

Exact Mass: 377.9803

 

Molecular Weight: 378.44

 

Elemental Analysis: C, 47.61; H, 2.66; N, 7.40; O, 16.91; S, 25.42

 

Synonym: 

 

CCF-642

CCF 642

CCF642

 

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

 

InChi Key: 

SPYIETQLOVDJCF-XYOKQWHBSA-N

 

InChi Code: InChI=1S/C15H10N2O4S3/c1-21-10-4-2-9(3-5-10)16-14(18)12(24-15(16)22)8-11-6-7-13(23-11)17(19)20/h2-8H,1H3/b12-8+

 

Smiles Code:

O=C1N(C2=CC=C(OC)C=C2)C(S/C1=C/C3=CC=C([N+]([O-])=O)S3)=S

 

 

Technical Data:

 

Appearance: Brown solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

CCF642 (3 μM; 0.5-6 hours) increases PERK dimerization by phosphorylation and IRE1-α oligomerization within 30 minutes in KMS-12-PE confirming accumulation of misfolded ER proteins.

CCF642, a bone marrow-sparing compound, exhibits a submicromolar IC50 in 10 of 10 multiple myeloma cell lines (MM1.S, MM1.R, KMS-12-PE, KMS-12-BM, NCI-H929, U266, RPMI 8226, JJN-3, HRMM.09-luc, 5TGM1-luc).

 

In Vivo:

CCF642 (10 mg/kg; i.p.; three times a week; for 24 days) significantly prolongs life of 5TGM1-luc-bearing mice and suppresses 5TGM1-luc growth as determined by life imaging.

 

 

References

 

  1. Vatolin S, Phillips JG, Jha BK, Govindgari S, Hu J, Grabowski D, Parker Y, Lindner DJ, Zhong F, Distelhorst CW, Smith MR, Cotta C, Xu Y, Chilakala S, Kuang RR, Tall S, Reu FJ. Novel Protein Disulfide Isomerase Inhibitor with Anticancer Activity in Multiple Myeloma. Cancer Res. 2016 Jun1 ; 76(11):3340-50. doi: 10.1158/0008-5472.CAN-15-3099. Epub 2016 Apr 6. PubMed PMID: 27197150.

 

Products are for research use only. Not for human use.

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