RET Inhibitor

HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia.

Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity.

ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC₅₀s of 2.1, 4.2, and 2.5 nM for ^V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers.

RET-IN-9 is a potent inhibitor of RET. RET kinase is a single-pass transmembrane receptor tyrosine kinase that plays an important role in the development of the kidney and enteric nervous system, and the maintenance of homeostasis in the nervous, endocrine, hematopoietic, and male reproductive systems. RET-IN-9 has the potential for the research of RET-related disease including non-small cell lung cancer and medullary thyroid cancer (extracted from patent WO2021115457A1, compound 29).

RET-IN-19 (compound 59) is a potent RET inhibitor, with IC₅₀ values of 6.8 and 13.51 nM against RET-wt and RET V804M, respectively. RET-IN-19 shows anticancer activity. RET-IN-19 can be used for non-small cell lung cancer (NSCLC) research.

RET-IN-26 (compound D5) is RET kinase inhibitor, with the IC₅₀ of 0.33 μM.

RET-IN-36 is an orally active RET kinase inhibitor. RET-IN-36 overcomes gatekeeper and solvent front resistance mutations and inhibits the proliferation of cells expressing RET^G810C and RET^V804M mutants by suppressing RET phosphorylation and SHC downstream signaling. RET-IN-36 can be used for research on RET-mutant cancers, medullary thyroid cancer, papillary thyroid cancer, and non-small cell lung cancer.

FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC₅₀ of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.

RET-IN-14 (compound 49) is a potent RET inhibitor with IC₅₀s of <0.51 nM, 9.3 nM, 1.3 nM, 9.2 nM, 15 nM for RET (WT), RET (G810R), RET (V804M), BTK and BTK (C481S), respectively. RET-IN-14 has the potential for tumors research

RET-IN-31 (Compound 13) is an orally active, selective RET inhibitor (IC₅₀s: 1.4 nM, 1.9 nM, 3.8 nM for RET^WT, RET^V804L, RET^V804M, respectively). RET-IN-31 inhibits hERG and Cytochrome P450 (IC₅₀s: 13.6 μM, 7.9 μM, 12.8 μM, 16.9 μM, 8.9 μM, 13.0 μM for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP3A4-M, CYP3A4-T, respectively). RET-IN-31 has anti-cancer effects against activated RET mutations and gene fusion-driven cancers.

KBP-7018 hydrochloride is an orally active, tyrosine kinase-selective multi-kinase inhibitor with an IC₅₀ value of 10 nM against c-KIT, 7.6 nM against RET, and 25 nM against human PDGFR. KBP-7018 hydrochloride improves survival rates in a mouse model of pulmonary fibrosis. KBP-7018 hydrochloride can be used in research related to idiopathic pulmonary fibrosis.

RET-IN-34 is a RET inhibitor with an IC₅₀ of 0.89 nM. RET-IN-34 serves as a target protein ligand for PROTAC synthesis (Ligand for Target Protein for PROTAC). RET-IN-34 is applicable for the synthesis of PROTAC RET Degrader 2 (HY-183783). RET-IN-34 exhibits anticancer activity against medullary thyroid carcinoma. RET-IN-34 can be used in studies related to medullary thyroid carcinoma.

Anti-GFRA4 Antibody is an anti-GFRA4 antibody. Recommend Isotype Controls: Human IgG1 kappa, Isotype Control (HY-P99001).

RET-IN-13 (compound 1), a quinoline compound, is a potent RET inhibitor with IC₅₀s of 0.5 nM, 0.9 nM for RET (WT) and RET (V804M), respectively. RET-IN-13 has the potential for tumors or intestinal diseases related to abnormal activation of RET research.

RET-IN-27 (compound 20p) is a potent inhibitor of RET, with IC₅₀s of 3.6 nM, 0.1 nM, 2.1 nM, 0.3 nM for RET^WT, RET^V804L, RET^V804M, RET^M918T, respectively. RET-IN-27 plays an important role in cancer research.

RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.

RET-IN-28 (Compound 16) is a RET (transmembrane receptor tyrosine protein kinase) inhibitor. RET-IN-28 inhibits the activity of the mutant RET enzyme (RET-V804M), and can be applied to cancer research.

RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC₅₀ values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC₅₀ 0.73 nM), V804L (IC₅₀ 0.36 nM), Y806H (IC₅₀ 0.74 nM) and M918T (IC₅₀ 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC₅₀ of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.

RET-IN-17 is a potent inhibitor of RET. RET-IN-17 has the potential for the research of pain associated with IBS and other gastrointestinal disorders and for the research of cancers with constitutive RET kinase activity (extracted from patent WO2016038552A1, compound 1).

RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC₅₀ of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects.