| DC70734 |
RET agonist BT44
|
RET agonist BT44 is a novel, specific RET agonist, promotes RET phosphorylation and selectively activates downstream cascades in the cells expressing GFL receptors.BT44 has no effect on TrkA and TrkB receptors; In GFRα1/RET expressing cells, 10–50 µM of BT44 increased the activity of luciferase reporter by approximately two fold (P<0.0001).BT44 dose-dependently stimulated neurite outgrowth from DRG sensory neurons and its efficacy was comparable to that of ARTN.BT44 alleviated mechanical hypersensitivity in surgery- and diabetes-induced rat models of neuropathic pain. |
| DC48424 |
Enbezotinib
|
Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer. |
| DC40968 |
LUN09945
|
LUN09945 is a potent RETV804M kinase inhibitor. LUN09945 was first reported by Rebecca Newton et al (Compound 13, in ACS Med Chem Lett. 2020;11(4):497-505). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature |
| DC11450 |
Selpercatinib(LOXO-292)
|
Selpercatinib 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. |
| DC7763 |
NVP-AST487
|
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. |
| DC11479 |
BLU-667 (Pralsetinib)
|
BLU-667 (Pralsetinib) is a highly potent, selective, next generation RET inhibitor with IC50 of 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion. |
| DC10633 |
AD80
|
AD80, a multikinase inhibitor, shows strong activity against human RET, BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM. |
| DC74420 |
HSN608
|
HSN608 (HSN 608) is a potent inhibitor of RET solvent-front mutants, inhibits RET G810 solvent-front mutants and the V804M gatekeeper mutant with IC50 of <50 nM in cell culture, inhibits ABL1(T315I) with IC50 of 40.7 nM. |
| DC72557 |
Pyrazoloadenine
|
Pyrazoloadenine is a potent RET (REarranged during Transfection) lung cancer oncoprotein inhibitor. Pyrazoloadenine shows anticancer activity. |
| DC70820 |
SYHA1815
|
SYHA1815 (SYHA-1815) is a novel potent, selective RET inhibitor, inhibits the kinase activity of RET wild type (IC50=0.9 nM) and V804 mutant (IC50=3.1 nM).SYHA1815 demonstrated approximately 20-fold selectivity for RET over KDR, exhibited a favorable selectivity profile, with> 100-fold selectivity over 347 kinases, and >10-fold selectivity over 44 other kinases in a panel of 395 kinases.SYHA1815 significantly inhibited RET phosphorylation and activation of its key adaptor protein SHC and the downstream signaling molecules p-AKT and p-ERK1/2 in classical RET mutant-driven MTC cell line TT (RETC634W), effectively inhibited p-RET, p-SHC, and downstream p-AKT and p-ERK activity.SYHA1815 inhibited RET-induced cell proliferation and overcame V804 mutants (TT cell proliferation IC50<1.6 nM), suppressed RET-driven cell proliferation via cell-cycle arrest through c-Myc downregulation.SYHA1815 showed potent antitumor efficacy against RET- and RET gatekeeper mutant-driven cancers in vivo. |
