Art. -Nr.: HY-124084A

SW203668 TFA

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SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC₅₀ of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer.

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Reinheit: 99.79%
CAS. Nr.: 2117405-48-6
Formel: C₂₄H₂₀F₃N₃O₄S
Molecular Weight:503.49

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

SW203668 TFA Chemical Structure

CAS. Nr.: 2117405-48-6

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

In Vitro

SW203668 (0.0003-6 μM) TFA selectively reduces viability of 4 human NSCLC cell lines with IC₅₀ values of 0.022, 0.031, 0.054, and 0.116 μM, and is non-toxic to 8 other human NSCLC cell lines^[1].
SW203668 (0.054 μM; 15 min pre-incubation, 30 min reaction) TFA inhibits SCD activity in H2122 cell microsomes with an IC₅₀ of 0.054 μM^[1].
SW203668 TFA is activated by CYP4F11 to induce toxicity in previously insensitive H1155 NSCLC cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SW203668 (compound 4) (6-25 mg/kg; i.p.; twice daily/once daily; 10-15/14 days) TFA substantially reduces the growth rate of CYP4F11-expressing H2122 non-small cell lung cancer xenografts in NOD-SCID mice at doses that spare sebocyte viability, demonstrating selective in vivo efficacy and reduced mechanism-related toxicity^[1].
SW203668 (6-20 mg/kg; i.p.; once daily; 15 days) TFA preserves sebocyte viability in healthy CD-1 mice at doses up to 20 mg/kg, avoiding the skin toxicity associated with conventional SCD inhibitors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD-SCID (male and female) injected with H2122 cells^[1]
Dosage:

25 mg/kg; 20 mg/kg; 6 mg/kg
Administration:

i.p.; twice daily (25 mg/kg); once daily (20, 6 mg/kg); 14-15 days
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

CAS. Nr. 2117405-48-6
Appearance Solid
Molecular Weight 503.49
Formel C₂₄H₂₀F₃N₃O₄S
Color White to off-white
SMILES

O=C(NC1=NC2=CC=C(OC)C=C2S1)C3=CC=C(C(N)C4=CC=CC=C4)C=C3.O=C(O)C(F)(F)F
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (198.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9861 mL

9.9307 mL

19.8614 mL

5 mM

0.3972 mL

1.9861 mL

3.9723 mL

10 mM

0.1986 mL

0.9931 mL

1.9861 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.97 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.97 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Theodoropoulos PC, et al. Discovery of tumor-specific irreversible inhibitors of stearoyl CoA desaturase. Nat Chem Biol. 2016;12(4):218-225. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	1.9861 mL	9.9307 mL	19.8614 mL	49.6534 mL
	5 mM	0.3972 mL	1.9861 mL	3.9723 mL	9.9307 mL
	10 mM	0.1986 mL	0.9931 mL	1.9861 mL	4.9653 mL
	15 mM	0.1324 mL	0.6620 mL	1.3241 mL	3.3102 mL
	20 mM	0.0993 mL	0.4965 mL	0.9931 mL	2.4827 mL
	25 mM	0.0794 mL	0.3972 mL	0.7945 mL	1.9861 mL
	30 mM	0.0662 mL	0.3310 mL	0.6620 mL	1.6551 mL
	40 mM	0.0497 mL	0.2483 mL	0.4965 mL	1.2413 mL
	50 mM	0.0397 mL	0.1986 mL	0.3972 mL	0.9931 mL
	60 mM	0.0331 mL	0.1655 mL	0.3310 mL	0.8276 mL
	80 mM	0.0248 mL	0.1241 mL	0.2483 mL	0.6207 mL
	100 mM	0.0199 mL	0.0993 mL	0.1986 mL	0.4965 mL

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SW203668 TFA

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SW203668 TFA

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Lipid Metabolism Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SW203668 TFA Related Classifications

Art. -Nr.: HY-124084A