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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-YAP-TEAD-SWTX-143
SWTX-143

Chemical Structure : SWTX-143

CAS No.: 2766575-48-6

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SWTX-143 (SWTX143)

货号: PC-21317Not For Human Use, Lab Use Only.

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

SWTX-143 is a potent, irreversible and covalent YAP/TAZ-TEAD inhibitor with IC50 of 12 nM in luciferase reporter assays, binds to the palmitoylation pocket of all four TEAD isoforms, inhibits Hippo pathway-mutant cancer cells.
SWTX-143 potently represses luciferase expression from the TEAD reporter (IC50=12 nmol/L) while not affecting the viability of HEK293 cells.
SWTX-143 is sufficient to evoke a long-lasting transcriptional impact.
SWTX-143 inhibits the proliferation of Hippo pathway-mutant cancer cell lines with IC50 of 5-207 nM against three distinct desothelioma cancer cell lines that are characterized by and depend on loss-of-function alterations in NF2 (Mero-14, NCI-H226, and CI-H2052) and one that is deficient in ATS1 and LATS2 (MSTO-211H).
SWTX-143 only modestly impacts the proliferation of the NCI-H28 and NCI-H2452 mesothelioma, HeLa, SiHa, and CaSki cancer cell lines which lack genetic alterations in known Hippo pathway components (Hippo-WT).
SWTX-143 (10, 25, and 50 mg/kg) causes regression of NF2-deficient human mesothelioma xenografts.
SWTX-143 also selectively impairs the growth of NF2-mutant kidney cancer cell lines, blocks Hippo pathway transcriptional output and causes tumor regression in preclinical mesothelioma models.

物理化学性质&存储条件

分子量 361.37
分子式 C19H18F3N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-[5-Amino-1,2,3,4-tetrahydro-1-[4-(trifluoromethyl)phenyl]-3-quinolinyl]-2-propenamide

参考文献

1. Hanne Hillen, et al. Mol Cancer Ther. 2023 Sep 23. doi: 10.1158/1535-7163.MCT-22-0681.

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