Home Protein Tyrosine Kinase EGFR inhibitor Lazertinib For research use only.

Lazertinib

Synonyms: YH25448,GNS-1480

Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.

Lazertinib Chemical Structure

Lazertinib Chemical Structure

CAS No. 1903008-80-9

Purity & Quality Control

Lazertinib Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
Targets
Del19/T790M [1]
(Cell-free assay)		 L858R/T790M EGFR [1]
(Cell-free assay)		 Del19 [1]
(Cell-free assay)		 L85R [1]
(Cell-free assay)		 WT EGFR [1]
(Cell-free assay)
1.7 nM 2 nM 5 nM 20.6 nM 76 nM
In vitro
In vitro

Lazertinib targets the activating EGFR mutations Del19 and L858R, as well as the T790M mutation, while sparing wild type. In NSCLC cell lines and primary cancer cells from patients harboring EGFR mutations, YH25448 more potently inhibits cancer cell growth and significantly increases tumor cell apoptosis compared to osimertinib[1]. In the cell proliferation assays, GI50 values of lazertinib are 6 nM, 5 nM, and 711 nM for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wt), respectively[2].
Cell Research Cell lines Ba/F3 cells
Concentrations 5, 10, 100 nM
Incubation Time 6 h
Method

Ba/F3 cells overexpressing the indicated EGFR mutant are treated with YH25448 or osimertinib for 6 hours at the indicated concentrations. pEGFR levels are detected by Western blot analysis.
In Vivo
In vivo

In an in vivo mouse model implanted with H1975 cells, once-daily YH25448 treatment results in indramatic dose-dependent tumor regression in both subcutaneous and intracranial lesions with no abnormal signs such as skin keratosis. The plasma half-life of YH25448 is 5.9-6.8 hr, while the tumor to plasma AUC0-last ratio is 3.0-5.1 in tumor-bearing mice. YH25448 shows excellent penetration of the blood-brain bartier, achieving CSF concentrations exceeding the IC50 value for pEGFR inhibition. YH25448 shows superior efficacy for tumor regression in an EGFR mutant brain metastasis model[1].
Animal Research Animal Models An intracranial tumor growth model (BALB/c nude mice inoculate with H1975-luc cells)
Dosages 10 and 25 mg/kg
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05896683 Completed
Healthy
Janssen Research & Development LLC
 May 30 2023 Phase 1
NCT05601973 Recruiting
Non Small Cell Lung Cancer
ETOP IBCSG Partners Foundation|Janssen Pharmaceuticals
 March 27 2023 Phase 2
NCT05742594 Completed
Healthy
Janssen Research & Development LLC
 January 3 2023 Phase 1
NCT05162274 Completed
Healthy Adult Volunteers
Yuhan Corporation
 November 30 2021 Phase 1
NCT05112952 Completed
Hepatic Impairment|Healthy
Janssen Research & Development LLC
 November 30 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 554.64 Formula

C30H34N8O3
CAS No. 1903008-80-9 SDF --
Smiles CN(C)CC1=CN(N=C1C2=CC=CC=C2)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N5CCOCC5)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 5 mg/mL ( (9.01 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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 Lazertinib | Lazertinib supplier | purchase Lazertinib | Lazertinib cost | Lazertinib manufacturer | order Lazertinib | Lazertinib distributor