RET (REarranged during Transfection) is a transmembrane receptor tyrosine kinase that is activated by a complex made up of a soluble GDNF family ligand (GFL) and a co-receptor that is glycosyl phosphatidylinositol-anchored (GFRalpha).
The enteric nervous system's development depends on RET signaling. The postnatal maintenance of dopaminergic neurons depends on RET, which also controls the development of sympathetic, parasympathetic, motor, and sensory neurons. Additionally, RET functions as a driver oncogene in a number of human cancers. In papillary thyroid, lung, colorectal, pancreatic, and breast cancers, RET has been found to fuse with a number of partner genes. Tyrosine kinase inhibitors (TKIs) for RET, particularly RET-specific inhibitors, show promising results against such cancers.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V69541 | Vepafestinib (TAS0953/HM06) | 2129515-96-2 | Vepafestinib (TAS0953/HM06; compound 6) is an inhibitor (blocker/antagonist) of RET (information from patent WO2019039439). |
|
V69542 | WF-47-JS03 | 2561413-77-0 | WF-47-JS03 is a potent and specific RET kinase inhibitor (antagonist) with over 500-fold selectivity over the kinase insert domain receptor (KDR). |
|
V4050 | WHI-P180 | 211555-08-7 | WHI-P180 (also known as Janex 3) is a multi-kinase inhibitor which inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively. |
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V69532 | Zeteletinib (BOS-172738; DS-5010) | 2216753-97-6 | Zeteletinib (BOS-172738; DS-5010) is an orally bioactive, selective RET kinase inhibitor (antagonist) with nanomolar potency for RET and >300-fold selectivity for VEGFR2. |
|
V69535 | Zeteletinib hemiadipate (BOS-172738 hemiadipate; DS-5010 hemiadipate) | 2375837-06-0 | Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally bioactive, selective RET kinase inhibitor (antagonist) with nanomolar potency for RET and >300-fold selectivity for VEGFR2. |
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