RET

Related Products

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.

RET Related Products (27):

By Effects:	Inhibitors (26) Agonists (1)

Cat. No.	Product Name	Effect	Purity

HY-10981

Lenvatinib	Inhibitor	99.74%
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities.

HY-10331

Regorafenib	Inhibitor	99.96%
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.

HY-112301

Pralsetinib	Inhibitor	99.56%
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (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.

HY-114370

Selpercatinib	Inhibitor	99.46%
Selpercatinib (LOXO-292) is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC₅₀ of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.

HY-10206

Amuvatinib	Inhibitor	99.36%
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

HY-133553

RET-IN-3 Inhibitor

RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC₅₀ of 19 nM.

RET-IN-3	Inhibitor
RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC₅₀ of 19 nM.

HY-133551

WF-47-JS03	Inhibitor
WF-47-JS03 is a potent RET kinase inhibitor with IC₅₀s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells, CCDC6-RET transfected LC-2/ad lung cancer cells, respectively.

HY-136534

RET V804M-IN-1 Inhibitor 98.37%

RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC₅₀ of 20 nM.
HY-18840

BBT594 Inhibitor 99.03%

BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.

RET V804M-IN-1	Inhibitor	98.37%
RET V804M-IN-1 (compound 5) is a wt-RET -selective inhibitors of RETV804M kinase, with an IC₅₀ of 20 nM.

BBT594	Inhibitor	99.03%
BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.

HY-10410

TG101209	Inhibitor	99.72%
TG101209 is a selective JAK2 inhibitor with IC₅₀ of 6 nM, less potent to Flt3 and RET with IC₅₀ of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.

HY-100459

GSK3179106	Inhibitor	99.78%
GSK3179106 is an orally active and selective RET kinase inhibitor with IC₅₀s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.

HY-15002

AST 487	Inhibitor	99.20%
AST 487 is a RET kinase inhibitor with IC₅₀ of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC₅₀ of 520 nM.

HY-13308

Regorafenib Hydrochloride	Inhibitor	99.58%
Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-101963

AD80 Inhibitor 99.46%

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

AD80	Inhibitor	99.46%
AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

HY-10331A

Regorafenib monohydrate	Inhibitor	99.96%
Regorafenib monohydrate is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC₅₀s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

HY-124401

BT-13	Agonist	>99.0%
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.

HY-16018A

Ilorasertib hydrochloride	Inhibitor	98.91%
Ilorasertib hydrochloride (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC₅₀s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC₅₀s of 7 nM, 3 nM and 32 nM, respectively.

HY-U00437

Pz-1 Inhibitor >99.0%

Pz-1 is a potent RET and VEGFR2 inhibitor with IC₅₀s of less than 1 nM for both wild type kinases.

Pz-1	Inhibitor	>99.0%
Pz-1 is a potent RET and VEGFR2 inhibitor with IC₅₀s of less than 1 nM for both wild type kinases.

HY-110193

SPP-86	Inhibitor	>99.0%
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.

HY-16018

Ilorasertib	Inhibitor
Ilorasertib (ABT-348) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC₅₀s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC₅₀s of 7 nM, 3 nM and 32 nM, respectively.

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