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c-Ret inhibitors act on RET, a receptor tyrosine kinase that guides neuronal and kidney development. The ret gene, short for rearranged during transfection, was described in 1985 as a transforming gene activated by DNA rearrangement. In 1996 RET was shown to transduce signals from glial cell line-derived neurotrophic factor (GDNF). Activating point mutations and RET gene fusions are studied in thyroid and lung tumor models. Selpercatinib and RPI-1 are inhibitors with RET as their main target, while BT-13 is described as a small-molecule RET agonist. Multikinase inhibitors such as regorafenib also block RET together with vascular endothelial growth factor receptors (VEGFR) and Raf kinases.
RET-IN-10 is a potent inhibitor of the receptor tyrosine kinase RET. Loss-of-function mutations in RET are linked to Hirschsprung's disease, whereas gain-of-function mutations are associated with various human malignancies. RET-IN-10 serves as a valuable tool for investigating the role of RET in cancer biology and for potential therapeutic applications in targeted cancer therapies.
Synonyms: TPX-0046 (enantiomer)
Enbezotinib (enantiomer) is a selective inhibitor of the RET (REarranged during Transfection) kinase, a critical target in various cancers. This compound demonstrates potent activity in inhibiting RET signaling pathways, making it a valuable tool for research into RET-dependent tumors. Its applications span studies in cancer biology, therapeutic development, and the exploration of resistance mechanisms in tumorigenesis.
RET ligand-2 is a selective inhibitor of the RET protein, primarily involved in oncogenic signaling pathways. It serves as a critical ligand for the development of PROTAC molecules aimed at degrading the RET protein, demonstrating potential antitumor activity. This compound can also be utilized in the synthesis of RD-23, facilitating research into targeted cancer therapies.
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RET-IN-8 is a selective inhibitor of the rearranged during transfection (RET) kinase, providing a valuable tool for cancer research. By targeting RET, this compound disrupts oncogenic signaling pathways associated with various malignancies. Its application in studying RET-driven tumors may facilitate the development of targeted therapies and enhance understanding of RET-related pathophysiology.
RET-IN-30 is a selective RET inhibitor, targeting both wild-type RET and several of its mutant forms. This compound demonstrates significant anti-proliferative activity in A549 cancer cells, highlighting its potential as an anti-tumor agent. RET-IN-30 is valuable for research focused on RET-related signaling pathways and targeted therapies in oncology.
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FHND5071 (1H) is a selective inhibitor of the RET (rearrangement during transfection) tyrosine kinase, making it a valuable tool for understanding RET-driven oncogenesis. This compound demonstrates significant biological activity against various cancers associated with RET alterations, including thyroid and lung cancers. FHND5071 (1H) is intended for research applications focused on elucidating RET signaling pathways and developing targeted therapeutic strategies.
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RET-IN-5 is a potent RET (rearranged during transfection) inhibitor, exhibiting an IC50 value of 0.4 nM against RET and 135.1 nM against VEGFR2. This compound is designed for research applications focusing on RET-mediated signaling pathways and its role in various cancers. Its selectivity and efficacy make it a valuable tool for understanding RET inhibition and its potential therapeutic implications.
RET-IN-18 is a potent inhibitor of the RET receptor tyrosine kinase, featuring a pyridone structure. This compound exhibits significant biological activity in the inhibition of RET signaling, making it a valuable tool for research into diseases associated with irritable bowel syndrome (IBS), gastrointestinal disorders, various cancers, and neurodegenerative diseases. Its application in these areas can facilitate the understanding of RET's role in disease mechanisms and potential therapeutic strategies.
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HG-6-63-01 is a type II inhibitor of the RET tyrosine kinase, specifically targeting the REarranged during Transfection (RET) kinase. This compound effectively impedes phosphorylation and signaling associated with oncogenic RET mutants, demonstrating significant activity in hindering the proliferation of fibroblasts transformed by RET/C634R and RET/M918T mutations. HG-6-63-01 shows promising potential for research applications focused on thyroid cancer and other malignancies driven by RET activation.
FHND5071 is a potent and selective inhibitor of the RET kinase, functioning primarily by blocking RET autophosphorylation. This mechanism of action results in significant antitumor effects, making FHND5071 a valuable tool for cancer research, particularly in studies focused on tumorigenic pathways involving RET signaling.
XMD15-44 is an inhibitor of RET kinase, a critical target in certain cancer signaling pathways. This compound exhibits a notable growth-inhibitory effect on RET/C634R and RET/M918T transformed RAT1 cells, with IC50 values of 11.5 nM and 8.3 nM, respectively. XMD15-44 effectively inhibits RET kinase activity and signaling in human thyroid cancer cell lines harboring oncogenic RET alleles, leading to a reduction in cell proliferation. Its specificity makes it a valuable tool for research into RET-related malignancies.
RET-IN-12 is a selective RET inhibitor, demonstrating potent inhibition with IC50 values of 0.3 nM for wild-type RET and 1 nM for the RET(V804M) mutant. This compound is valuable for research in cancer biology, particularly in studies targeting neuroendocrine tumors and specific RET-driven malignancies. Its effectiveness in inhibiting both wild-type and mutant RET makes it an important tool for investigating RET-related signaling pathways and therapeutic responses.
