[CAS NO. 346640-08-2] CCF642
PRODUCTS SPECIFICATIONS [346640-08-2]
DESCRIPTION [346640-08-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 378.45 |
| Molecular Formula | C15H10N2O4S3 |
| SMILES | O=C1N(C2=CC=C(OC)C=C2)C(S/C1=C/C3=CC=C([N+]([O-])=O)S3)=S |
Summary
CCF642 is a potent protein disulfide isomerases (PDI) inhibitor with an IC 50 of 2.9 μM. CCF642 causes acute endoplasmic reticulum (ER) stress in multiple myeloma cells accompanied by apoptosis-inducing calcium release. CCF642 has broad anti-multiple myeloma activity [1] .
IC50 & Target
IC50: 2.9 μM (PDI) [1]
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
[1]
.
CCF642, a bone marrow-sparing compound, exhibits a submicromolar IC
50
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)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| 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. |
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/KaLwRij mice of 6 to 8 weeks of age with 5TGM1-luc [1] |
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 30 mg/mL ( 79.27 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.6424 mL | 13.2118 mL | 26.4236 mL |
| 5 mM | 0.5285 mL | 2.6424 mL | 5.2847 mL |
| 10 mM | 0.2642 mL | 1.3212 mL | 2.6424 mL |
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1.