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.
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.
Apatinib (YN968D1) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM. Apatinib (YN968D1) also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib (YN968D1) inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ.
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.
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.
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.
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.
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.
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.
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.
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.
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.
Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the treatment of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ.
cis-Pralsetinib (cis-BLU-667) is a highly potent and selective inhibitor of rearranged during transfection (RET), with IC50s ranging from 0.3 to 0.4 nM for WT RET and four enzyme variants (V804L, V804M, M918T, CCDC6-RET), and with broad, robust and anti-tumor activity against multiple RET-driven solid tumor types.
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