c-RET

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβべーた and is orally active. Regorafenib has antitumor and anti-angiogenic activity.

Fedratinib (TG-101348) (TG101348) is an ATP-competitive inhibitor of JAK2 (IC50: 3 nM) with significantly less potent activity against JAK3.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

Compound TPX-0046 is an inhibitor of RET. Compound TPX-0046 can inhibit the RET autophosphorylation. Compound TPX-0046 can be used for the research of cancer.

DUN73423 (RET-IN-21) is a potent tyrosine kinase (RET) inhibitor with antitumour activity for the study of cancer.

TG-89 is an inhibitor of JAK2, JAK3, RET and FLT3, and has an IC50 value of 11.2 μみゅーM against JAK2, showing anticancer activity in the treatment of ovarian and cervical cancer.

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

AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.

Danusertib (PHA-739358) is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.

Selpercatinib (LOXO-292) is a tyrosine kinase inhibitor with antineoplastic properties(IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively)

Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.

WHI-P180 (Janex 3) is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A/Aurora B/Aurora C (IC50s: 120 nM/7 nM/1 nM). It also suppresses RET tyrosine kinase, PDGFRβべーた, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-βべーた, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6 1.9 6.2 nM).

TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.

Enbezotinib is an inhibitor of RET autophosphorylation and can be used in cancer research.

TAS05567 is a potent, highly selective, and ATP-competitive Syk inhibitor (IC50: 0.37 nM). TAS05567 only shows >70% inhibition of Syk and 4 other kinases (FLT3, JAK2, KDR, and RET with IC50s of 10 nM, 4.8 nM, 600 nM, and 29 nM, respectively) in a panel of 192 kinases.

trans-Pralsetinib (trans-BLU-667) is an inhibitor of rearranged during transfection (RET).

ON123300 is a potent and multi-targeted kinase inhibitor for CDK4/Ark5/PDGFRβべーた/FGFR1/RET/Fyn (IC50: 3.9/5/26/26/9.2/11 nM).

Regorafénib N-oxyde M2 is an active metabolite of Regorafenib. Regorafenib is a multi-target inhibitor for VEGFR1/2/3, PDGFRβべーた, RET, Kit, and Raf-1 (IC50s: 13/4.2/46, 1.5, 22, 7, and 2.5 nM).

Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

RET-IN-3 is a RETV804M kinase inhibitor with potential anticancer activity for the study of non-small cell lung cancer.

Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.

SPP-86 is an effective and selective cell-permeable inhibitor of RET tyrosine kinase with an IC50 of 8 nM.

RET V804M-IN-1 (RETV804M kinase inhibitor) is a wt-RET -selective RETV804M kinase inhibitors(IC50 = 20 nM).

BT-13 is a selective agonist of glial cell line-derived neurotrophic factor (GDNF) receptor RET independently of GFLs. BT-13 promotes neurite growth from sensory neurons in vitro.

BBT594 (NVP-BBT594)(NVP-BBT594) is a potent inhibitor of receptor tyrosine kinase RET,Treatment of cancer.

PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.

ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRαあるふぁ.

Vepafestinib is a RET inhibitor with potential antineoplastic activity[1].

TPX-0046 is a RET inhibitor designed to overcome resistance to Selpercatinib and Pralsetinib.

Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).

RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.