CS47
Based on 1 Customer Validation
CS47 is a Thioredoxin Reductase 1 (TRXR1) inhibitor and ferroptosis inducer. CS47 binds non-covalently to sites between the FAD and NADPH pockets of TRXR1. CS47 drives glutathione depletion, lipid reactive oxygen species accumulation, HMOX1-dependent iron overload, and selective cytotoxicity in lung cancer cells. CS47 can be used for the research of lung cancer.
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- Pureza : 95.0%
- No. CAS: 1372792-51-2
- Fòrmula: C21H16AuCl2N2P
- Peso molecular:595.21
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
In Vitro
CS47 (48 h) selectively reduces viability of KRAS-WT and EGFR-MUT human lung cancer cells in 2D culture with IC50 values of 6.74 µM and 6.78 µM, respectively, while showing much lower potency against KM lung cancer cells (IC50 = 24.22 µM) and normal IMR90 fibroblasts (IC50 = 54.85 µM)[1].
CS47 (48 h) induces potent cell death in 3D spheroids of KRAS-WT (H661, H522) and EGFR-MUT (HCC827) human lung cancer cells, but not in KM (H460) or KRAS-WT H522 cells with KM overexpression[1].
CS47 (2 μM; 24 h) induces significant lipid peroxidation in KRAS-WT human lung cancer cells (H1993, H1395), but not in KRASG12C human lung cancer cells (H157, A549)[1].
CS47 (2 μM; 24 h) alters lipid homeostasis in KRAS-WT H522 human lung cancer cells, inducing enrichment of ferroptosis-associated PUFA-containing phospholipids and accumulation of LPC and PUFA-containing TG[1].
CS47 (24 h) induces transcriptomic reprogramming in KRAS-WT and EGFR-MUT human lung cancer cells, downregulating lipid biosynthesis and selenoprotein genes while upregulating ferroptosis-related genes involved in antioxidant response, iron metabolism, and GSH homeostasis; HMOX1 is universally upregulated across all genotypes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUClast | Vz/F | CL/F | MRT |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 20.33 μg/mL | 90 min | 3803 min | 23737567 min·ng/mL | 538 mL/kg | 0.098 mL/min/kg | 686 min |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG (Nod Scid IL-2Rγ-/-) mice (9 weeks) injected with H661 and H661-HMOX1 cells[1]
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Dosage:3 mg/kg
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Administration:i.p.; every 3 days; 25 days
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Result:Produced a significant anti-tumor effect, with tumor volumes remaining far lower than vehicle controls throughout the 25-day treatment period.
Increased intratumoral C11-BODIPY oxidation, a marker of lipid peroxidation.
Induced accumulation of polyunsaturated fatty acid-containing phospholipids and triacylglycerols, consistent with ferroptosis.
Did not cause significant weight loss in mice.
Exhibited no marked leukopenia or neutropenia observed.
Exhibited even more pronounced anti-tumor effect in H661-HMOX1-GFPlo xenografts.
Increased intratumoral accumulation of 4-Hydroxynonenal, a marker of ferroptosis, in both parental and HMOX1-overexpressing xenografts.
Chemical Information
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No. CAS 1372792-51-2
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Appearance Solid
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Peso molecular 595.21
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Fòrmula C21H16AuCl2N2P
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Color Off-white to light yellow
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SMILES
ClC1=C(Cl)[N-]([Au+][P](C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4)C=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (168.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6801 mL | 8.4004 mL | 16.8008 mL | 42.0020 mL |
| 5 mM | 0.3360 mL | 1.6801 mL | 3.3602 mL | 8.4004 mL | |
| 10 mM | 0.1680 mL | 0.8400 mL | 1.6801 mL | 4.2002 mL | |
| 15 mM | 0.1120 mL | 0.5600 mL | 1.1201 mL | 2.8001 mL | |
| 20 mM | 0.0840 mL | 0.4200 mL | 0.8400 mL | 2.1001 mL | |
| 25 mM | 0.0672 mL | 0.3360 mL | 0.6720 mL | 1.6801 mL | |
| 30 mM | 0.0560 mL | 0.2800 mL | 0.5600 mL | 1.4001 mL | |
| 40 mM | 0.0420 mL | 0.2100 mL | 0.4200 mL | 1.0500 mL | |
| 50 mM | 0.0336 mL | 0.1680 mL | 0.3360 mL | 0.8400 mL | |
| 60 mM | 0.0280 mL | 0.1400 mL | 0.2800 mL | 0.7000 mL | |
| 80 mM | 0.0210 mL | 0.1050 mL | 0.2100 mL | 0.5250 mL | |
| 100 mM | 0.0168 mL | 0.0840 mL | 0.1680 mL | 0.4200 mL |
CS47 Related Classifications
HY-175806 Related Classifications
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