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LOXO-292 (Selpercatinib) RET Inhibitor

Name: LOXO-292 (Selpercatinib)
Brand: Selleck Chemicals
SKU: S8781
Availability: InStock
Rating: 5 (11 reviews)

Cat.No.S8781

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.

Chemical Structure

Molecular Weight: 525.60

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other c-RET Inhibitors	AD80 GSK3179106 YW-N-7 TFA TPX-0046

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (47.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.100mg/ml (7.80mM)	Taking the 1 mL working solution as an example, add 50 μL 82 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	525.60	Formula	C₂₉H₃₁N₇O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2152628-33-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ARRY-192			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

Mechanism of Action

Targets/IC₅₀/Ki	RET wt (Cell-free assay) 1 nM RET V804M (Cell-free assay) 2 nM RET V804L (Cell-free assay) 2 nM RET M918T (Cell-free assay) 2 nM RET S891A (Cell-free assay) 2 nM RET A883F (Cell-free assay) 4 nM
In vitro	Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor.
References	[1] https://www.loxooncology.com/docs/presentations/2016_EORTC_LOXO-292_POSTER.pdf [2] https://pubmed.ncbi.nlm.nih.gov/33921066/ [3] https://pubmed.ncbi.nlm.nih.gov/31988000/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pRET / Flag / cPARP / Actin		33161056

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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