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 |
|---|---|---|---|---|
|
V3376 | AST487 (NVP- AST487) | 630124-46-8 | AST487 (also known as NVP- AST487) is a novel and potent inhibitor of RET kinase with anticancer activity. |
|
V4663 | BBT-594 | 882405-89-2 | BBT-594 (also known as NVP-BBT594) is a novel, potent and selective receptor tyrosine kinase RET inhibitor used for cancer treatment. |
|
V69553 | Enbezotinib (enantiomer) (TPX-0046 (enantiomer)) | 2359650-19-2 | Enbezotinib (Enantiomer) (Compound 44) is the enantiomeric form of enbezotinib. |
|
V69549 | FHND5071 | 2761152-16-1 | FHND5071 is a potent and specific RET kinase inhibitor. |
|
V3552 | GSK3179106 | 1627856-64-7 | GSK3179106 is a novel, potent, selective, and gut-restricted RET kinase inhibitorwith anIC50of 0.4 nM. |
|
V98077 | HG-6-63-01 | 2177298-99-4 | HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). |
|
V69539 | NSC194598 | 5358-76-9 | NSC194598 is a p53 DNA binding inhibitor (antagonist) with IC50s of 180 nM and 2-40 μM for inhibiting p53 sequence-specific DNA binding in vitro and in vivo, respectively. |
|
V4830 | Pralsetinib (BLU 667) | 2097132-94-8 | Pralsetinib (GAVRETO; BLU667; BLU-667) is a novel, highly potent, selective, FDA approved RET inhibitor with anticancer activity. |
|
V69544 | Pyrazoloadenine | 2380-63-4 | Pyrazoloadenine is a potent inhibitor of the RET lung cancer oncoprotein. |
|
V69547 | RET-IN-22 | 2918281-79-3 | RET-IN-22 (compound 17b) is a specific, orally bioactive RET inhibitor (antagonist) with IC50s of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. |
|
V69551 | RET-IN-23 | 2479961-46-9 | RET-IN-23 (compound 17) is a potent orally bioactive RET inhibitor (antagonist) with IC50s of 1.32 and 2.50 for RET-WT, RET-CCDC6, RET-V804L, RET-V804M, and RET-M918T respectively. |
|
V69554 | RET-IN-24 | 2583767-68-2 | RET-IN-24 (Compound 26) is a selective RET tyrosine kinase inhibitor (TKI) (antagonist) with anti-tumor activity. |
|
V69540 | RET-IN-25 | 2965703-02-8 | RET-IN-25 (compound 6b) is a RET kinase inhibitor (antagonist) with anti-cancer activity. |
|
V79251 | RET-IN-26 | RET-IN-26 (compound D5) is a RET kinase inhibitor (antagonist) with IC50 of 0.33 μM. | |
|
V94406 | RET-IN-27 | RET-IN-27 (Compound 20p) is a potent inhibitor of RET with IC50 of 3.6 nM, 0.1 nM, 2.1 nM and 0.3 nM for RETWT, RETV804L, RETV804M and RETM918T, respectively. | |
|
V69543 | RET-IN-3 | 2414374-53-9 | RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor (antagonist) with IC50 of 19 nM. |
|
V51535 | RET-IN-4 | 2436473-55-9 | RET inhibitor |
|
V69545 | RET-IN-5 | 2725770-20-5 | RET-IN-5 is a potent RET inhibitor (antagonist) with IC50 of 4.57 nM (WO2021213476A1, compound 18). |
|
V69550 | RET-IN-6 | 2715208-83-4 | RET-IN-6 is a potent RET inhibitor (antagonist) with IC50 of 4.57 nM (CN113461670A, compound 321). |
|
V69546 | RET-IN-7 | 2763386-05-4 | RET-IN-7 displays potent RET kinase inhibition in vitro and potent efficacy against RET-driven tumor xenografts in vivo. |
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