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RET

RET

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.

RET related products

Structure Cat No. Product Name CAS No. Product Description
AST487 (NVP- AST487) 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.
BBT-594 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.
Enbezotinib (enantiomer) (TPX-0046 (enantiomer)) V69553 Enbezotinib (enantiomer) (TPX-0046 (enantiomer)) 2359650-19-2 Enbezotinib (Enantiomer) (Compound 44) is the enantiomeric form of enbezotinib.
FHND5071 V69549 FHND5071 2761152-16-1 FHND5071 is a potent and specific RET kinase inhibitor.
GSK3179106 V3552 GSK3179106 1627856-64-7 GSK3179106 is a novel, potent, selective, and gut-restricted RET kinase inhibitorwith anIC50of 0.4 nM.
NSC194598 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.
Pralsetinib (BLU 667) 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.
Pyrazoloadenine V69544 Pyrazoloadenine 2380-63-4 Pyrazoloadenine is a potent inhibitor of the RET lung cancer oncoprotein.
RET-IN-22 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.
RET-IN-23 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.
RET-IN-24 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.
RET-IN-25 V69540 RET-IN-25 2965703-02-8 RET-IN-25 (compound 6b) is a RET kinase inhibitor (antagonist) with anti-cancer activity.
RET-IN-26 V79251 RET-IN-26 RET-IN-26 (compound D5) is a RET kinase inhibitor (antagonist) with IC50 of 0.33 μM.
RET-IN-3 V69543 RET-IN-3 2414374-53-9 RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor (antagonist) with IC50 of 19 nM.
RET-IN-4 V51535 RET-IN-4 2436473-55-9 RET inhibitor
RET-IN-5 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).
RET-IN-6 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).
RET-IN-7 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.
RET/TRKA-IN-1 V87855 RET/TRKA-IN-1 RET/TRKA-IN-1 (Compound 13) is a dual inhibitor of RET (IC50=0.375 µM) and TRKA. RET/TRKA-IN-1 inhibits the cell viability of LC-2 and KM12 cells with GI50 of 0.72 and 0.25 μM, respectively.
RETV804M kinase inhibitor V2168 RETV804M kinase inhibitor 2414909-94-5 RETV804M kinase inhibitor (Compound 13) is a novel and potent inhibitor of RETV804M kinase, which is the anticipated drug-resistant mutant of RET kinase.
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