2. Metabolic Enzyme/Protease
  3. Stearoyl-CoA Desaturase (SCD)
  4. SW203668 TFA

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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SW203668 TFA

SW203668 TFA Chemical Structure

CAS No. : 2117405-48-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
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10 mM * 1 mL in DMSO In-stock
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5 mg In-stock
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Based on 1 publication(s) in Google Scholar

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SW203668 TFA Related Antibodies

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  • Purity & Documentation

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Description

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[1].

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.

SW203668 TFA Related Antibodies
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.
Molecular Weight

503.49

Formula

C24H20F3N3O4S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9861 mL 9.9307 mL 19.8614 mL
5 mM 0.3972 mL 1.9861 mL 3.9723 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.79%

SDS (251 KB)

COA (250 KB) HNMR (282 KB) LCMS (103 KB)

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. 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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SW2036682117405-48-6SW 203668SW-203668Stearoyl-CoA Desaturase (SCD)immunodeficient miceCYP4F11mouse skin sebocyteshuman stearoyl CoA desaturaseunsaturated fatty acidsSCDH2122 cell microsomesNSCLC cellsNSCLC xenograftsnon-small cell lung cancerInhibitorinhibitorinhibit

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