SW203668
Based on 1 Customer Validation
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer.
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- CAS No.: 1673556-40-5
- 화학식: C22H19N3O2S
- 분자량:389.47
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H2122 | IC50 |
22 nM
Compound: rac-27
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Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
Inhibition of SCD in human NCI-H2122 cells expressing CYP4F11 assessed as reduction in cell viability incubated for 96 hrs by cell titer Glo reagent based assay
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[PMID: 32787093] |
In Vitro
SW203668 is selectively cytotoxic to 4 human NSCLC cell lines (H2122, H460, and 2 others) with IC50 values of 0.022-0.116 μM, and shows no toxicity to 8 other human NSCLC cell lines at concentrations up to 10 μM[1].
SW203668 inhibits SCD activity in H2122 cell microsomes with an IC50 of 0.054 μM[1].
SW203668 is activated by CYP4F11 to crosslink and inhibit SCD, conferring cytotoxicity to previously insensitive H1155 NSCLC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 25 mg/kg | i.p. | 8 h |
In Vivo
SW203668 (6-20 mg/kg; i.p.; once daily; 15 days) spares sebocyte viability in healthy CD-1 mice at daily i.p. doses of 6 mg/kg and 20 mg/kg for 15 days, with 20 mg/kg showing significantly higher sebocyte counts than a conventional SCD inhibitor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (male and female) injected with H2122 cells[1]
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Dosage:25 mg/kg; 20 mg/kg; 6 mg/kg
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Administration:i.p.; twice daily (25 mg/kg); once daily (20, 6 mg/kg); 14-15 days
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Result:Substantially reduced the growth rate of H2122-derived tumors at 25 mg/kg twice daily for 10-15 days.
Showed no effect on H1155-derived tumors at 25 mg/kg twice daily for 10-15 days.
Inhibited H2122 tumor growth at 20 mg/kg once daily for 14 days.
Resulted in significantly higher sebocyte counts in mouse skin than Xenon-45 at 20 mg/kg once daily for 14 days.
Maintained a therapeutic window with preserved sebocytes at 6 mg/kg once daily for 14 days.
- RNA extraction experimental
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Patient-Derived Orthotopic Xenograft (PDOX)
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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CAS No. 1673556-40-5
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Appearance Solid
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분자량 389.47
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화학식 C22H19N3O2S
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SMILES
COC1=CC=C2C(SC(NC(C3=CC=C(C=C3)C(C4=CC=CC=C4)N)=O)=N2)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
In Vitro:
DMSO : 50 mg/mL (128.38 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 (protect from light). 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 (protect from light). 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (273 KB)
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SDS (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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Handling Instructions (2659 KB)
References
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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5676 mL | 12.8380 mL | 25.6759 mL | 64.1898 mL |
| 5 mM | 0.5135 mL | 2.5676 mL | 5.1352 mL | 12.8380 mL | |
| 10 mM | 0.2568 mL | 1.2838 mL | 2.5676 mL | 6.4190 mL | |
| 15 mM | 0.1712 mL | 0.8559 mL | 1.7117 mL | 4.2793 mL | |
| 20 mM | 0.1284 mL | 0.6419 mL | 1.2838 mL | 3.2095 mL | |
| 25 mM | 0.1027 mL | 0.5135 mL | 1.0270 mL | 2.5676 mL | |
| 30 mM | 0.0856 mL | 0.4279 mL | 0.8559 mL | 2.1397 mL | |
| 40 mM | 0.0642 mL | 0.3209 mL | 0.6419 mL | 1.6047 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL | 1.2838 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4279 mL | 1.0698 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3209 mL | 0.8024 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL |
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