Selpercatinib (Synonyms: LOXO-292)

Name: Selpercatinib
Brand: MedChemExpress
SKU: HY-114370
Rating: 5.0 (11 reviews)

Cat. No.: HY-114370 Purity: 99.83%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 2152628-33-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Selpercatinib:

11 Publications Citing Use of MCE Selpercatinib

Cell Proliferation/Viability Assay

2D/3D Cell Culture and Differentiation

In Vivo Efficacy Study

: 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.

: Selpercatinib purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2021 Apr 15;13(8):1909.; 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.; Treatment with two different RET TKIs (Selpercatinib (LOXO292) (1 μM, 24 h) or BLU667) blocked RA-induced differentiation.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Purity & Documentation
References
Customer Review

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	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	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	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	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	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]
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]

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

Molecular Weight

525.60

Formula

C₂₉H₃₁N₇O₃

CAS No.

2152628-33-4

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.83%

Select Batch:

Data Sheet (277 KB) SDS (393 KB)

COA (253 KB) LCMS (110 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.

Complete Stock Solution Preparation Table

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

Selpercatinib Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Selpercatinib2152628-33-4LOXO-292LOXO292LOXO 292RETanticancerRET (WT)RET (V804M)RET (G810R)FVB/NRj miceInhibitorinhibitorinhibit

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Selpercatinib (Synonyms: LOXO-292)

Customer Review

Other Forms of Selpercatinib:

Selpercatinib Related Antibodies

11 Publications Citing Use of MCE Selpercatinib

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Selpercatinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report