Cat. No.: HY-138751

limertinib

(Synonyms: ASK120067)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

limertinib (ASK120067) is a potent and orally active inhibitor of EGFR^T790M (IC₅₀:0.3 nM) with selectivity over EGFR^WT (IC₅₀:6.0 nM). limertinib is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC).

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Pureté: 99.12%
CAS No.: 1934259-00-3
Formule: C₂₉H₃₂ClN₇O₂
Masse moléculaire:546.06

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

limertinib Chemical Structure

CAS No.: 1934259-00-3

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

EGFR^T790M

0.5 nM (IC₅₀)

EGFR^L858R/T790M

0.3 nM (IC₅₀)

EGFR (WT)

6 nM (IC₅₀)

EGFR^{Exon 19 deletion}

0.5 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform EGFR :

In Vitro

In the in vitro kinase assay limertinib potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC₅₀ values of 0.3 nM and 0.5 nM, respectively, as well as the EGFR^exon19del sensitizing mutant (IC₅₀= 0.5 nM). The ₅₀ of limertinib against wild-type EGFR (EGFR^WT) is 6 nM^[1].
limertinib selectively inhibits the growth of EGFR-mutant cell lines and exhibits potent antiproliferative activity in the mutant EGFR NSCLC cells, with IC₅₀ values of 12 nM, 6 nM and 2 nM against NCI-H1975 (T790M mutation), PC-9, and HCC827 cells (sensitizing mutations), respectively. However, it shows moderate or weak anti-growth activities in A431, LoVo and A549 cells (EGFR^WT), with IC₅₀ values ranging from 338 nM to 1541 nM^[1].
limertinib (0.1-100 nM) inhibits the phosphorylation of EGFR at Tyrosine residue 1068 and its downstream signaling proteins AKT and ERK in NCI-H1975 cells (EGFR^L858R/T790M) even at low dosage (0.1-1 nM). Additionally, limertinib inhibits p-EGFR and p-Akt and p-erk in EGFR WT A431 cell until the concentration reaches 10 to 100 nM^[1].

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

In Vivo

limertinib (oral gavage; 5-20 mg/kg; once daily; 21 days) results in significantly regressed tumor growth, with a tumor growth inhibition (TGI) rate of 85.7%, and administration of 10 mg/kg limertinib causes dramatic tumor shrinkage with a TGI rate of 99.3%, exhibiting a similar potency with Osimertinib^[1].

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

Animal Model:

BALB/cA nude mice^[1]
Dosage:

5-20 mg/kg
Administration:

Oral gavage; 5-20 mg/kg; once daily; 21 days
Result:

Were well tolerated in animals without observed body weight loss
Demonstrated profound and selective antitumor efficacy and decreased TGI rate.
Significantly inhibited the phosphorylation of EGFR L858R/T790M and AKT in tumor tissue.

Chemical Information

CAS No. 1934259-00-3
Appearance Solid
Masse moléculaire 546.06
Formule C₂₉H₃₂ClN₇O₂
Color White to yellow
SMILES

O=C(NC1=CC(NC2=NC=C(C(NC3=CC4=C(C=CC=C4)C=C3)=N2)Cl)=C(C=C1N(CCN(C)C)C)OC)C=C
Synonyms

ASK120067
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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Journal Impact Factor

NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
J Med Chem

Profiling and Optimizing Targeted Covalent Inhibitors through EGFR-Guided Studies. [Abstract]

2025 Aug 28;68(16):17917-17932. PMID: 40801664

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (183.13 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

1.8313 mL

9.1565 mL

18.3130 mL

5 mM

0.3663 mL

1.8313 mL

3.6626 mL

10 mM

0.1831 mL

0.9157 mL

1.8313 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.58 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. Tao Zhang, et al. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8313 mL	9.1565 mL	18.3130 mL	45.7825 mL
	5 mM	0.3663 mL	1.8313 mL	3.6626 mL	9.1565 mL
	10 mM	0.1831 mL	0.9157 mL	1.8313 mL	4.5783 mL
	15 mM	0.1221 mL	0.6104 mL	1.2209 mL	3.0522 mL
	20 mM	0.0916 mL	0.4578 mL	0.9157 mL	2.2891 mL
	25 mM	0.0733 mL	0.3663 mL	0.7325 mL	1.8313 mL
	30 mM	0.0610 mL	0.3052 mL	0.6104 mL	1.5261 mL
	40 mM	0.0458 mL	0.2289 mL	0.4578 mL	1.1446 mL
	50 mM	0.0366 mL	0.1831 mL	0.3663 mL	0.9157 mL
	60 mM	0.0305 mL	0.1526 mL	0.3052 mL	0.7630 mL
	80 mM	0.0229 mL	0.1145 mL	0.2289 mL	0.5723 mL
	100 mM	0.0183 mL	0.0916 mL	0.1831 mL	0.4578 mL

Keywords

limertinib

2 Cited Publications

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limertinib

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Publications Citing Use of MedChemExpress (MCE) limertinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

limertinib Related Classifications

HY-138751 Related Classifications