RET

RET (REarranged during Transfection) is a receptor protein tyrosine kinase, which activates multiple signal transduction pathways. RET protein is composed of three domains: an extracellular ligand-binding domain, a transmembrane domain, and a cytoplasmic tyrosine kinase domain. The RET receptor tyrosine kinase (RTK) regulates key aspects of cellular proliferation and survival by regulating the activity of the mitogen- activated protein kinase (MAPK) and PI3K/Akt signaling pathways. RET also interacts directly with other kinases such as the epidermal growth factor receptor (EGFR) and hepatocyte growth factor receptor (MET) and the focal adhesion kinase (FAK). Furthermore, BRAF and p38MAPK are downstream targets of RET. Kinase inhibitors that simultaneously inhibit RET and its downstream targets.

RET tyrosine kinase receptor presents an attractive therapeutic target for the treatment of certain cancer subsets. Deregulated RET activity has been identified as a causative factor in the development, progression and response to therapy of thyroid carcinoma. Elevated RET expression has been associated with the development of endocrine resistance in human breast cancer.

Targets for RET

Products for RET

Cat.No. Product Name Information
GC68623 AD57
AD57 is a type of orally active multi-kinase inhibitor that inhibits the activity of RET, BRAF, S6K and Src, but has significantly reduced activity against mTOR.
GC32797 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
GC16391 Amuvatinib (MP-470, HPK 56)

HPK56, MP470
A multi-targeted RTK inhibitor
GC33362 Amuvatinib hydrochloride (MP470 hydrochloride)

MP470 hydrochloride; HPK 56 hydrochloride
Amuvatinib hydrochloride (MP470 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) (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
GC14292 Apatinib Mesylate

YN968D1
Apatinib Mesylate blocks the downstream signal transduction of VEGF pathway to inhibit neovascularization.
GC60592 APS6-45 APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
GC10914 AST 487

NVP-AST 487
A multi-kinase inhibitor
GC19062 BBT594

NVP-BBT594
BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.
GC34509 BT-13 BT-13 is a potent and selective glial cell line-derived neurotrophic factor (GDNF) receptor RET agonist independently of GFLs, promoting neurite growth from sensory neurons in vitro and attenuates experimental neuropathy in the Rat.
GC68812 BT44
BT44 is a selective RET activator. It can penetrate the blood-brain barrier and can be used for research on neurodegenerative diseases and diabetes.
GC65354 Enbezotinib Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer.
GC18492 GSK3179106

RET Kinase Inhibitor 1
A RET kinase inhibitor
GC34159 Ilorasertib (ABT-348)

ABT-348
Ilorasertib (ABT-348) (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib (ABT-348) also is a potent VEGF, PDGF inhibitor. Ilorasertib (ABT-348) has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
GC38519 Ilorasertib hydrochloride

ABT-348 hydrochloride
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS).
GC15454 Lenvatinib (E7080)

E-7080, ER-203492-00
E7080, known as lenvatinib, is an oral multitargeted tyrosine kinase inhibitor including VEGF, FGF and SCF receptors that has been shown to improve the survival rate of patients with radioiodine-refractory thyroid cancer.
GC36438 Lenvatinib mesylate

E-7080
An inhibitor of VEGFR2 and VEGFR3
GC49686 N-desmethyl Regorafenib N-oxide An active metabolite of regorafenib
GC31780 Pralsetinib (Blu667) Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (Blu667) (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively.
GC37047 Pz-1 Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.
GC10111 Regorafenib

BAY 73-4506
A multi-kinase inhibitor
GC14606 Regorafenib hydrochloride A multi-kinase inhibitor
GC14534 Regorafenib monohydrate A multi-kinase inhibitor
GC73196 RET-IN-21 RET-IN-21 is an inhibitor of receptor tyrosine kinase (RET), with the IC50 of 4.4 μM, that has antitumor activity.
GC67917 RET-IN-7
GC33192 Selpercatinib A RET kinase inhibitor
GC34809 SPP-86 SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
GC10035 TG101209 An inhibitor of JAK2, FLT3, RET, and JAK3
GC68396 Vepafestinib
GC37933 WHI-P180 hydrochloride

Janex 3 hydrochloride;
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
GC64340 Zeteletinib

BOS-172738; DS-5010
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity.