SW203668
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:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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] |
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.
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 25 mg/kg | i.p. | 8 h |
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.
Chemical Information
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CAS No. 1673556-40-5
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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
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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Data Sheet (270 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SW203668 Related Classifications
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