Home Apoptosis c-RET inhibitor Selpercatinib (LOXO-292) For research use only.

Selpercatinib (LOXO-292)

Synonyms: ARRY-192

Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.

Selpercatinib (LOXO-292) Chemical Structure

Selpercatinib (LOXO-292) Chemical Structure

CAS No. 2152628-33-4

Purity & Quality Control

Selpercatinib (LOXO-292) Related Products

Signaling Pathway

c-RET Signaling Pathways

c-RET Signaling Pathway

Biological Activity

Description Selpercatinib (LOXO-292, ARRY-192) is a potent and specific RET (c-RET) inhibitor with IC50 values of 1 nM, 2 nM, 2 nM, 4 nM, 2 nM, 2 nM for WT RET, RET V804M, RET V804L, RET A883F, RET M918T and RET S891A respectively.
Targets
RET wt [1]
(Cell-free assay)		 RET V804M [1]
(Cell-free assay)		 RET V804L [1]
(Cell-free assay)		 RET M918T [1]
(Cell-free assay)		 RET S891A [1]
(Cell-free assay)		 Click to View More Targets
1 nM 2 nM 2 nM 2 nM 2 nM
In vitro
In vitro

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor.
Cell Research Cell lines NB1 cells
Concentrations 1 μM
Incubation Time 2 h
Method

Cells were pre-treated with LOXO292 (1 µM) for 2 h before stimulation with ALKAL2 or GDNF.
Experimental Result Images Methods Biomarkers Images PMID
Western blot pRET / Flag / cPARP / Actin 33161056
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05324124 Completed
Healthy
Loxo Oncology Inc.|Eli Lilly and Company
 April 19 2022 Phase 1
NCT05136404 Completed
Healthy
Loxo Oncology Inc.|Eli Lilly and Company
 December 3 2021 Phase 1
NCT05089019 Completed
Healthy
Loxo Oncology Inc.|Eli Lilly and Company
 October 29 2021 Phase 1
NCT04782076 Completed
Healthy
Loxo Oncology Inc.|Eli Lilly and Company
 March 5 2021 Phase 1
NCT04280081 Active not recruiting
Solid Tumor|Medullary Thyroid Cancer
Loxo Oncology Inc.|Eli Lilly and Company
 March 16 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 525.60 Formula

C29H31N7O3
CAS No. 2152628-33-4 SDF --
Smiles CC(C)(COC1=CN2C(=C(C=N2)C#N)C(=C1)C3=CN=C(C=C3)N4CC5CC(C4)N5CC6=CN=C(C=C6)OC)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 25 mg/mL ( (47.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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