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Cat.No. Product Name Information Product Use Citations Product Validations
S8401 Erdafitinib (JNJ-42756493) Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. This compound also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis.
Commun Biol, 2025, 8(1):394
Int J Mol Sci, 2025, 26(8)3525
J Clin Invest, 2024, 134(2)e169241
Verified customer review of Erdafitinib (JNJ-42756493)
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
Cell Rep Med, 2025, S2666-3791(25)00231-9
Cell Rep, 2024, 43(7):114446
J Cell Sci, 2021, jcs.258685
S1164 E7080 (Lenvatinib) Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3.
Nature, 2025, 10.1038/s41586-025-08585-z
Drug Resist Updat, 2025, 81:101224
Nat Cancer, 2025, 10.1038/s43018-025-01058-2
Verified customer review of E7080 (Lenvatinib)
S8716 Pralsetinib (BLU-667) Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).
J Exp Clin Cancer Res, 2025, 44(1):154
J Pharm Biomed Anal, 2025, 266:117078
Elife, 2024, 12RP89100
S8781 LOXO-292 (Selpercatinib) Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.
J Exp Clin Cancer Res, 2025, 44(1):154
Toxicol Appl Pharmacol, 2025, 500:117393
J Pharm Biomed Anal, 2025, 266:117078
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but was much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Nat Commun, 2022, 13(1):2500
Mol Cancer Res, 2020, 18(8):1176-1188
Mol Cancer Res, 2020, 1176-1188
S8821 GSK3179106 GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and this compound is efficacious in vivo.
Respir Res, 2024, 25(1):388
E8288New YW-N-7 TFA YW-N-7 TFA is a PROTAC that targets the inhibition and degradation of RET with a DC50 of 88 nM. It also exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse model.
S9826 TPX-0046

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.
S1178 Regorafenib (BAY 73-4506) Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.
Nat Commun, 2025, 16(1):509
Cell Death Differ, 2025, 10.1038/s41418-025-01536-1
Cell Mol Gastroenterol Hepatol, 2025, S2352-345X(25)00026-8
Verified customer review of Regorafenib (BAY 73-4506)

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