Enbezotinib|CAS 2359649-81-1|DC Chemicals

Cas No.:	2359649-81-1
Chemical Name:	Enbezotinib
SMILES:	FC1=CC(CN2[C@H](CCC3)[C@H]3OC(C2=N4)=CN5C4=C6C=N5)=C(O[C@@H](C)CNC6=O)N=C1
Formula:	C₂₁H₂₁FN₆O₃
M.Wt:	424.43
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[1]. ROGERS EW, et, al. Macrocyclic compounds for treating disease. WO2019126121A1.

Description:	Enbezotinib, an inhibitor of RET, can inhibit the RET autophosphorylation. Enbezotinib can be used for the research of cancer[1].
In Vivo:	Enbezotinib (compound 5) (2-5 mg/kg; twice daily for 27 days) decreases tumor size in mice[1].
In Vitro:	Enbezotinib (compound 5) (0.3-300 nM) inhibits p-RET (y905) in RET-driven cells[1].
References:	[1]. ROGERS EW, et, al. Macrocyclic compounds for treating disease. WO2019126121A1.

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.