RET agonist BT44

  Cat. No.:  DC70734   Featured
Chemical Structure
924759-42-2
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Cas No.: 924759-42-2
Chemical Name: RET agonist BT44
SMILES: O=C(N1CCN(C2=CC(S(=O)(N3CC4=C(C=CC=C4)CC3)=O)=CC=C2OC)CC1)C5=CC=C(F)C=C5C(F)(F)F
Formula: C28H27F4N3O4S
M.Wt: 577.595
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
References: 1. Viisanen H, et al. Mol Pain. 2020 Jan-Dec;16:1744806920950866. 2. Renko JM, et al. J Parkinsons Dis. 2021;11(3):1023-1046.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
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.
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