| Chemical Properties | Back Directory | [Boiling point ]
578.662±50.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.336±0.10 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
13.963±0.20(predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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 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]. | 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. |
| [IC 50]
YAP/TAZ-TEAD | [References]
[1] Hanne Hillen, et al. A novel irreversible TEAD inhibitor, SWTX-143, blocks Hippo pathway transcriptional output and causes tumor regression in preclinical mesothelioma models. Mol Cancer Ther. 2023 Sep 23. DOI:10.1158/1535-7163.MCT-22-0681 |
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