Cat. No.: HY-114370

Selpercatinib

(Synonyms: LOXO-292)

12 Cited Publications

Customer Review

Based on 12 publication(s) in Google Scholar

Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC₅₀ values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity.

For research use only. We do not sell to patients.

Purity: 99.83%
CAS No.: 2152628-33-4
Formula: C₂₉H₃₁N₇O₃
Molecular Weight:525.60

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Selpercatinib Chemical Structure

CAS No.: 2152628-33-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 14.0 nM (RET^WT), 24.1 nM (RET^V804M), and 530.7 nM (RET^G810R)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	10.6 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	1102 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810R-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	1242 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810C incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	17.4 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	253 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810S incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	37.8 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	4340 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804L-G810R incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	472 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase G810C-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	7.4 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing wildtype rearranged during transfection kinase-CCDC6 incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	72 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells expressing rearranged during transfection kinase V804M-KIF5B incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	>10000 nM Compound: 5	Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method Antiproliferative activity against mouse BaF3 cells incubated for 74 to 76 hrs by cell counting kit 8 method	[PMID: 36308779]
BaF3	IC₅₀	0.01 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	0.02 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-V804L mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-V804L mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	0.1 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-V804M mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-V804M mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	0.26 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810A mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810A mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	0.4 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810S mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810S mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	2.1 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810R mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810R mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]
BaF3	IC₅₀	5.8 μM Compound: Selpercatinib	Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810C mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay Cytotoxicity against mouse BaF3 cells expressing KI5B-RET kinase-G810C mutant fusion protein assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay	[PMID: 39291010]

In Vivo

Selpercatinib (LOXO-292; 10 mg/kg; i.g.; for 0-2 h) has good pharmacokinetics after oral gavage in FVB/NRj mice^[1].
Pharmacokinetic Parameters of Selpercatinib in FVB/NRj mice^[1].

Administration	i.g. (10 mg/kg)
T_max (h)	1.8
C_max (ng/mL)	7862
AUC (ng·h/mL)	26649

FVB/NRj mice, 10 mg/kg i.g.^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male FVB/NRj mice^[1]
Dosage:

10 mg/kg
Administration:

Oral gavage; for 7.5 min, 15 min, 30 min, 1 h and 2 h (Pharmacokinetic Analysis)
Result:

Had good pharmacokinetics after oral gavage in FVB/NRj mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2152628-33-4
Appearance Solid
Molecular Weight 525.60
Formula C₂₉H₃₁N₇O₃
Color White to off-white
SMILES

N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OCC(C)(O)C)=CN2N=C1
Synonyms

LOXO-292
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All WBCell Proliferation/Viability Assay2D/3D Cell Culture and DifferentiationIn Vivo Efficacy Study

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Journal Impact Factor

Cancer Biol Ther

RET fusion partners dictate oncogenic potential in undifferentiated spindle cell sarcomas. [Abstract]

2026 Dec 31;27(1):2683190. PMID: 42240026
Molecules

Assessment of In Silico and In Vitro Selpercatinib Metabolic Stability in Human Liver Microsomes Using a Validated LC-MS/MS Method. [Abstract]

2023 Mar 14;28(6):2618. PMID: 36985590
Cancers (Basel)

Loss of RET Promotes Mesenchymal Identity in Neuroblastoma Cells. [Abstract]

2021 Apr 15;13(8):1909. PMID: 33921066

Selpercatinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2021 Apr 15;13(8):1909. [Abstract]

Western blot analysis of RET immunoprecipitates (IPs) from NB1 cells treated with combinations of either ALKAL2, glial cell line-derived neurotrophic factor (GDNF), crizotinib, or Selpercatinib (LOXO292) (1 μM) as indicated. Phospho-RET antibodies were used to indicate RET activation, and blots reprobed with RET antibody were used as control.

Selpercatinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2021 Apr 15;13(8):1909. [Abstract]

Treatment with two different RET TKIs (Selpercatinib (LOXO292) (1 μM, 24 h) or BLU667) blocked RA-induced differentiation.
Curr Issues Mol Biol

Loss of WT1 Drives Adaptive Plasticity in CCDC6-RET Selpercatinib-Resistant Papillary Thyroid Cancer. [Abstract]

2026 Mar 4;48(3):274. PMID: 41899426
Biol Open

A Functional sgRNA-CRISPR screening method for generating murine RET and NTRK1 rearranged oncogenes. [Abstract]

2023 Aug 15;12(8):bio059994. PMID: 37470475

Selpercatinib purchased from MedChemExpress. Usage Cited in: Biol Open. 2023 Aug 15;12(8):bio059994. [Abstract]

TR.1 cells were seeded at 200 cells/well in 96-well plates and after 24 h, treated for 7 days with Selpercatinib (LOXO-292) (0-300 nM) or BLU-667 at the indicated concentrations. Cell number was determined with CyQUANT reagent as described in the Materials and Methods.

Selpercatinib purchased from MedChemExpress. Usage Cited in: Biol Open. 2023 Aug 15;12(8):bio059994. [Abstract]

Tumor shrinkage was induced by Selpercatinib (LOXO-292) (10 mg/kg, i.g.) treatment after 6 (31.4 + 9.1%) and 13 (27.4 + 5.2%) days of treatment.
Biomed Chromatogr

Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]

2024 Oct;38(10):e5986. PMID: 39136165
Biomed Chromatogr

Development and validation of an HPLC-MS/MS method to simultaneously quantify brigatinib, lorlatinib, pralsetinib and selpercatinib in human K2-EDTA plasma. [Abstract]

2023 Jun;37(6):e5628. PMID: 36941218
Drug Discov Ther

Development of a simple high-performance liquid chromatography-ultraviolet detection method for selpercatinib determination in human plasma. [Abstract]

2025 Jan 14;18(6):387-390. PMID: 39647867
bioRxiv

2025 April 26.
Maastricht University

2023 Jun 1.
Syddansk Universitet

2023 May 22.
bioRxiv

A Rapid, Functional sgRNA Screening Method for Generating Murine RET and NTRK1 Fusion Oncogenes. [Abstract]

2023 Apr 6:2023.04.06.535912. PMID: 37066347

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (118.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9026 mL

9.5129 mL

19.0259 mL

5 mM

0.3805 mL

1.9026 mL

3.8052 mL

10 mM

0.1903 mL

0.9513 mL

1.9026 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Şentürk R, et, al. Quantitative bioanalytical assay for the selective RET inhibitors selpercatinib and pralsetinib in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2020 Jun 15;1147:122131. [Content Brief]

[2]. Steven W. Andrews, et al. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors. WO2018071447A1.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9026 mL	9.5129 mL	19.0259 mL	47.5647 mL
	5 mM	0.3805 mL	1.9026 mL	3.8052 mL	9.5129 mL
	10 mM	0.1903 mL	0.9513 mL	1.9026 mL	4.7565 mL
	15 mM	0.1268 mL	0.6342 mL	1.2684 mL	3.1710 mL
	20 mM	0.0951 mL	0.4756 mL	0.9513 mL	2.3782 mL
	25 mM	0.0761 mL	0.3805 mL	0.7610 mL	1.9026 mL
	30 mM	0.0634 mL	0.3171 mL	0.6342 mL	1.5855 mL
	40 mM	0.0476 mL	0.2378 mL	0.4756 mL	1.1891 mL
	50 mM	0.0381 mL	0.1903 mL	0.3805 mL	0.9513 mL
	60 mM	0.0317 mL	0.1585 mL	0.3171 mL	0.7927 mL
	80 mM	0.0238 mL	0.1189 mL	0.2378 mL	0.5946 mL
	100 mM	0.0190 mL	0.0951 mL	0.1903 mL	0.4756 mL

Keywords

Selpercatinib

12 Cited Publications

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Selpercatinib

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Publications Citing Use of MedChemExpress (MCE) Selpercatinib

Biological Activity

Chemical Information

Publications (12)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Selpercatinib Related Classifications

HY-114370 Related Classifications