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CCF642

Cat. No. M8686
CCF642 Structure
Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 130  USD130 In stock
25mg USD 260  USD260 In stock
50mg USD 460  USD460 In stock
100mg USD 660  USD660 In stock
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Quality Control & Documentation
Biological Activity

CCF642 is a cell-permeable protein disulfide isomerase (PDI) inhibitor that exhibits 100-fold higher potency than PACMA 31 (by di-E-GSSG assay) via an alternative mode of action that most likely involves PDI active-site CGHCK motifs instead of cysteine known to be targeted by PACMA 31. CCF642 displays anti-multiple myeloma (MM) activity both in cultures in vitro (IC50 <1 μM against murine 5TGM1 and nine human MM lines) and in mice in vivo (10 mg/kg, 3X i.p. per wk) without apparent adverse effects to the animals or being cytotoxic to normal bone marrow (NLBM) cells even at concentrations as high as 6.75 μM. Consistent with PDI′s role in ER protein folding process, CCF642 treatment causes acute ER stress accompanied by apoptosis-inducing calcium release in MM cells.

Chemical Information
Molecular Weight 378.45
Formula C15H10N2O4S3
CAS Number 346640-08-2
Form Solid
Solubility (25°C) DMSO: 5 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Metis Hasipek, et al. Therapeutic Targeting of Protein Disulfide Isomerase PDIA1 in Multiple Myeloma

[2] Xiaohan Gao, et al. Extracellular vesicles derived from oesophageal cancer containing P4HB promote muscle wasting via regulating PHGDH/Bcl-2/caspase-3 pathway

[3] Maryam Kamarehei, et al. Inhibition of protein disulfide isomerase has neuroprotective effects in a mouse model of experimental autoimmune encephalomyelitis

[4] Sergei Vatolin, et al. Novel Protein Disulfide Isomerase Inhibitor with Anticancer Activity in Multiple Myeloma

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