2. Stem Cell/Wnt
  3. YAP
  4. SWTX-143

SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity.

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SWTX-143 Chemical Structure

SWTX-143 Chemical Structure

CAS No. : 2766575-48-6

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Based on 1 publication(s) in Google Scholar

SWTX-143 Related Antibodies

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Description

SWTX-143 is an orally active YAP/TAZ-TEAD inhibitor that binds to the palmitoylation pocket of all four TEAD isoforms. SWTX-143 causes irreversible and specific inhibition of the transcriptional activity of YAP/TAZ-TEAD and shows antitumor activity[1].

In Vitro

SWTX-143 (5-207 nM, 6 days) inhibits the proliferation of NF2-deficient mesothelioma cells, with IC50 values ranging from 5 to 207 nM[1].
SWTX-143 (12 nM, 24 hours) selectively inhibits TEAD transcription factor activity in HEK293 cells, with an IC50 of 12 nM[1].

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

SWTX-143 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: NCI-H226, NCI-H2052, Mero-14 (NF2-deficient mesothelioma cell lines)
Concentration: 5 to 207 nM
Incubation Time: 6 days
Result: Inhibited proliferation in NF2-deficient mesothelioma cells.
In Vivo

SWTX-143 (10, 25, 50 mg/kg, p.o., once daily for 19 days) induces dose-dependent tumor reduction in the NCI-H226 xenograft nude mouse model without notable side effects[1].

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

Animal Model: NF2-deficient human mesothelioma (NCI-H226) xenograft BALB/c nude mice model
Dosage: 10, 25, and 50 mg/kg
Administration: Oral gavage (p.o.), once daily for 19 days
Result: Had little effect on tumor volume during the first week of dosing;
Resulted in significant dose-dependent reduction in tumor volume observed afterward;
Led to no significant weight loss at the end of dosing.
Molecular Weight

361.36

Formula

C19H18F3N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C=C)NC1CC2=C(N)C=CC=C2N(C3=CC=C(C(F)(F)F)C=C3)C1
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 : 125 mg/mL (345.92 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 2.7673 mL 13.8366 mL 27.6732 mL
5 mM 0.5535 mL 2.7673 mL 5.5346 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.

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Purity & Documentation
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 2.7673 mL 13.8366 mL 27.6732 mL 69.1831 mL
5 mM 0.5535 mL 2.7673 mL 5.5346 mL 13.8366 mL
10 mM 0.2767 mL 1.3837 mL 2.7673 mL 6.9183 mL
15 mM 0.1845 mL 0.9224 mL 1.8449 mL 4.6122 mL
20 mM 0.1384 mL 0.6918 mL 1.3837 mL 3.4592 mL
25 mM 0.1107 mL 0.5535 mL 1.1069 mL 2.7673 mL
30 mM 0.0922 mL 0.4612 mL 0.9224 mL 2.3061 mL
40 mM 0.0692 mL 0.3459 mL 0.6918 mL 1.7296 mL
50 mM 0.0553 mL 0.2767 mL 0.5535 mL 1.3837 mL
60 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1531 mL
80 mM 0.0346 mL 0.1730 mL 0.3459 mL 0.8648 mL
100 mM 0.0277 mL 0.1384 mL 0.2767 mL 0.6918 mL
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SWTX-143 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:

SWTX-1432766575-48-6SWTX143SWTX 143YAPYes-associated proteinYAP/TAZ-TEAD InhibitorCancerInhibitorinhibitorinhibit

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