RET Inhibitor

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

Regorafenib (BAY 73-4506) 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 shows very robust antitumor and antiangiogenic activity.

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

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC₅₀ values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity.

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.

RET-IN-32 is an orally active RET inhibitor with IC₅₀ values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer.

GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC₅₀ values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD⁺ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.

Cofetuzumab (PF-06523435) is a humanized IgG1-κ monoclonal antibody targeting PTK7. The expression system of Cofetuzumab is typically CHO (Chinese hamster ovary) cells. Cofetuzumab downregulates PTK7 expression, modulates its downstream signaling pathways, and inhibits tumor sphere formation of ovarian cancer cells. Cofetuzumab can be used to synthesize the ADC molecule Cofetuzumab pelidotin (HY-P99829). Cofetuzumab is applicable to the research of tumors such as ovarian cancer.

PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a K_i of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

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.

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.

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 Hydrochloride (BAY 73-4506 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.

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.

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

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

NSC194598 is a p53 DNA-binding inhibitor with an IC₅₀ value of 180 nM. NSC194598 inhibits p53 DNA binding and induction of target genesn when p53 is stabilized and activated by irradiation or chemotherapy. NSC194598 can interfere with transcriptional activation of mutated rearranged during transfection (RET) gene, induce apoptosis and G0/G1 phase arrest. NSC194598 can be used for the researches of acute radiation toxicity and medullary thyroid carcinoma.

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.

Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC₅₀ value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas.

CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC₅₀ of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive.