RET
RET (REarranged during Transfection) is a transmembrane receptor tyrosine kinase that is activated by a complex consisting of a soluble glial cell line-derived neurotrophic factor (GDNF) family ligand (GFL) and a glycosyl phosphatidylinositol-anchored co-receptor, GDNF family receptors alpha (GFRalpha).
RET signalling is crucial for the development of the enteric nervous system. RET regulates the development of sympathetic, parasympathetic, motor, and sensory neurons, and is necessary for the postnatal maintenance of dopaminergic neurons. RET also plays a role as a driver oncogene in a variety of human cancers. Fusion of RET with several partner genes has been detected in papillary thyroid, lung, colorectal, pancreatic, and breast cancers, and tyrosine kinase inhibitors (TKIs) for RET (particularly RET-specific inhibitors) show promising effects against such cancers.
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RET Related Products (160)
Related Products (160)
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APS03118
0 ImagesCat. No.: HY-178061CAS No.: 2598870-24-5APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research.
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Regorafenib-d3
0 ImagesSynonyms: BAY 73-4506-d3Regorafenib-d3 (BAY 73-4506-d3) is a deuterium labeled Regorafenib (HY-10331). Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor.
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JNJ-38158471
0 ImagesCat. No.: HY-18317CAS No.: 951151-97-6JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
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Regorafenib mesylate
0 ImagesCat. No.: HY-10331BCAS No.: 835621-08-4Synonyms: BAY 73-4506 mesylateRegorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.
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Amuvatinib hydrochloride
0 ImagesCat. No.: HY-10206ACAS No.: 1055986-67-8Synonyms: MP470 hydrochloride; HPK 56 hydrochlorideAmuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
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Zeteletinib hemiadipate
0 ImagesCat. No.: HY-139590ACAS No.: 2375837-06-0Synonyms: BOS-172738 hemiadipate; DS-5010 hemiadipateZeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity.
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RET-IN-4
0 ImagesCat. No.: HY-132193CAS No.: 2436473-55-9RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.
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RET V804E Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70777Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET V804E is a mutant of RET. RET V804E Recombinant Human Active Protein Kinase is a recombinant RET V804E protein that can be used to study RET V804E-related functions.
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CLM3
0 ImagesCat. No.: HY-164413CAS No.: 1312024-59-1CLM3, a pyrazolopyrimidine derivative, is a multiple tyrosine kinase inhibitor. CLM3 shows antiproliferative and proapoptotic activity on endothelial and cancer cells, synergistically enhanced by SN38 (HY-13704). These effects are mainly due to its inhibition of phosphorylation of VEGFR-2, EGFR and RET tyrosine kinases and their related signaling pathways.
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RET-IN-15
0 ImagesCat. No.: HY-144422CAS No.: 2643375-86-2
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RET L790F Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70859Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET L790F is a mutant of RET. RET L790F Recombinant Human Active Protein Kinase is a recombinant RET L790F protein that can be used to study RET L790F-related functions.
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Lenvatinib-d5
0 ImagesCat. No.: HY-10981S1Synonyms: E7080-d5
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RET L730I Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70771Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET L730I is a mutant of RET. RET L730I Recombinant Human Active Protein Kinase is a recombinant RET L730I protein that can be used to study RET L730I-related functions.
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RET S891A Recombinant Human Active Protein Kinase
0 ImagesCat. No.: HY-E70776Rearranged during transfection (RET) is a transmembrane receptor protein tyrosine kinase (PTK) activated normally by forming ternary complexes with its cognate ligands and co-receptors. RET alterations by point mutations and gene fusions were found in diverse cancers. RET S891A is a mutant of RET. RET S891A Recombinant Human Active Protein Kinase is a recombinant RET S891A protein that can be used to study RET S891A-related functions.
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Lenvatinib-15N,d4
0 ImagesCat. No.: HY-10981S2Purity: 98.01%Synonyms: E7080-15N,d4Lenvatinib-15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.
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QZ2135
0 ImagesCat. No.: HY-170852QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854).
