1603845-42-6
Chemical Structure
TX2-121-1
- CAS No.: 1603845-42-6
- Formula:C42H52N8O3
- Molecular Weight:716.91
IUPAC Name: (R)-N-(2-(4-(3-(3-acrylamido-4-phenoxyphenyl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)ethyl)-4-((3R,5R,7R)-adamantan-1-yl)-2-methylbutanamide
InChIKey: GKJWHLDKQULMHJ-VIQSTUIZSA-N
SMILES: C[C@@H](C(NCCN1CCC(N2C3=NC=NC(N)=C3C(C(C=C4)=CC(NC(C=C)=O)=C4OC5=CC=CC=C5)=N2)CC1)=O)CCC6(C[C@H](C7)C8)C[C@H]8C[C@H]7C6
Biological Activity: TX2-121-1 is a bifunctional hydrophobic tag Her3 degrader and also a Her3 inhibitor with an IC50 of 49 nM. TX2-121-1 covalently binds to Cys721 of Her3, induces Her3 degradation via the Hsp70/Hsp90-assisted proteasomal pathway, interferes with the heterodimerization of Her3 with Her2/c-Met, and attenuates downstream Erk/Akt signaling, thereby inhibiting Her3-dependent cancer cell growth. TX2-121-1 can be used for the research of non-small cell lung cancer, ovarian cancer and Her3-driven breast cancer[1][2][3][4][5][6].
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TX2-121-1 | TX2-121-1 is a bifunctional hydrophobic tag Her3 degrader and also a Her3 inhibitor with an IC50 of 49 nM. TX2-121-1 covalently binds to Cys721 of Her3, induces Her3 degradation via the Hsp70/Hsp90-assisted proteasomal pathway, interferes with the heterodimerization of Her3 with Her2/c-Met, and attenuates downstream Erk/Akt signaling, thereby inhibiting Her3-dependent cancer cell growth. TX2-121-1 can be used for the research of non-small cell lung cancer, ovarian cancer and Her3-driven breast cancer. | |||||||||||||||||||||
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References
- [1]. Lim SM, et al. Development of small molecules targeting the pseudokinase Her3. Bioorganic & medicinal chemistry letters. 2015 Aug 15;25(16):3382-9. [Content Brief]
- [2]. Li H, et al. Protein degradation technology: a strategic paradigm shift in drug discovery. Journal of hematology & oncology. 2021 Sep 06;14(1):138.
- [3]. Xie T, et al. Pharmacological targeting of the pseudokinase Her3. Nature chemical biology. 2014 Dec;10(12):1006-12. [Content Brief]
- [4]. Xie S, et al. Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation. Journal of medicinal chemistry. 2023 Aug 24;66(16):10917-10933. [Content Brief]
- [5]. Lai AC, et al. Induced protein degradation: an emerging drug discovery paradigm. Nature reviews. Drug discovery. 2017 Feb;16(2):101-114.
- [6]. Zhang N, et al. HER3/ErbB3, an emerging cancer therapeutic target. Acta biochimica et biophysica Sinica. 2016 Jan;48(1):39-48.
