2857937-59-6
Chemical Structure
MYF-03-176
- CAS No.: 2857937-59-6
- Formula:C19H18F4N4O2
- Molecular Weight:410.37
IUPAC Name: 2-fluoro-1-((3R,4R)-3-(pyrimidin-2-ylamino)-4-((4-(trifluoromethyl)benzyl)oxy)pyrrolidin-1-yl)prop-2-en-1-one
InChIKey: KVAWNRUJSYWYJX-HZPDHXFCSA-N
SMILES: FC(F)(F)C1=CC=C(CO[C@@H]2CN(C(C(F)=C)=O)C[C@H]2NC3=NC=CC=N3)C=C1
Biological Activity: MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model[1][2][3].
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MYF-03-176 | 99.72% | MYF-03-176 is an orally active inhibitor of TEAD, and suppresses TEAD transcriptional activity with an IC50 of 11 nM. The IC50 values of MYF-03-176 for TEAD1, TEAD3, and TEAD4 are 47, 32, and 71 nM, respectively. MYF-03-176 inhibits hippo signaling defective malignant pleural mesothelioma (MPM) cells. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model. | ||||||||||||||||||||
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- [1]. Mengyang Fan, et al. Covalent Disruptor of YAP-TEAD Association Suppresses Defective Hippo Signaling. BioRxiv.
- [2]. Lu W, et al. Structure-Based Design of Y-Shaped Covalent TEAD Inhibitors. J Med Chem. 2023 Apr 13;66(7):4617-4632. [Content Brief]
- [3]. Yang W, et al. YAP/TAZ mediates resistance to KRAS inhibitors through inhibiting proapoptosis and activating the SLC7A5/mTOR axis. JCI Insight. 2024 Dec 20;9(24):e178535. [Content Brief]
Keywords
