Selpercatinib (LOXO-292)

Catalog No.S8781 Synonyms: ARRY-192

For research use only.

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

CAS No. 2152628-33-4

Selleck's Selpercatinib (LOXO-292) has been cited by 2 Publications

Purity & Quality Control

Choose Selective c-RET Inhibitors

Other c-RET Products

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
Assay
Methods Test Index PMID
Western blot pRET / Flag / cPARP / Actin 33161056

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 525.60
Formula

C29H31N7O3

CAS No. 2152628-33-4
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05324124 Completed Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company April 19 2022 Phase 1
NCT05136404 Completed Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company December 3 2021 Phase 1
NCT05089019 Active not recruiting Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company October 29 2021 Phase 1
NCT04782076 Completed Drug: Dabigatran|Drug: Selpercatinib Healthy Loxo Oncology Inc.|Eli Lilly and Company March 5 2021 Phase 1
NCT04320888 Recruiting Drug: Selpercatinib Hematopoietic and Lymphoid Cell Neoplasm|Recurrent Ependymoma|Recurrent Ewing Sarcoma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Lymphoma|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Glioma|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Recurrent WHO Grade 2 Glioma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Lymphoma|Refractory Malignant Germ Cell Tumor|Refractory Malignant Glioma|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Refractory WHO Grade 2 Glioma|Wilms Tumor National Cancer Institute (NCI)|Children''s Oncology Group September 14 2020 Phase 2
NCT04280081 Active not recruiting Drug: Selpercatinib Solid Tumor|Medullary Thyroid Cancer Loxo Oncology Inc.|Eli Lilly and Company March 16 2020 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Selpercatinib (LOXO-292) | Selpercatinib (LOXO-292) supplier | purchase Selpercatinib (LOXO-292) | Selpercatinib (LOXO-292) cost | Selpercatinib (LOXO-292) manufacturer | order Selpercatinib (LOXO-292) | Selpercatinib (LOXO-292) distributor