Referencia número: HY-109061

Lazertinib

(Synonyms: YH25448; GNS-1480)

3 Cited Publications

Revisión del cliente

Based on 3 publication(s) in Google Scholar

Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC₅₀ values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

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Pureza: 99.87%
No. CAS: 1903008-80-9
Fòrmula: C₃₀H₃₄N₈O₃
Peso molecular:554.64

Almacenamiento:

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

Lazertinib Chemical Structure

No. CAS: 1903008-80-9

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (3)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

EGFR^T790M

TRPA1

Ver todos los productos específicos de isoformas EGFR :

Ver todos los productos específicos de isoformas TRP Channel :

Ver todos los productos específicos de isoformas Akt :

Ver todos los productos específicos de isoformas ERK :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	3.6 μM Compound: 5; YH25448	Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
BaF3	EC₅₀	>100 nM Compound: YH25448	Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	EC₅₀	4.8 nM Compound: YH25448	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
BaF3	EC₅₀	7.4 nM Compound: YH25448	Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay	[PMID: 36518696]
NCI-H1975	IC₅₀	<1 μM Compound: 5; YH25448	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]
U-87MG ATCC	IC₅₀	33.2 μM Compound: 5; YH25448	Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay	[PMID: 31869655]

In Vitro

Lazertinib (0.1-1000 nM; 3 d) inhibits the viability of Ba/F3 cells expressing various rare EGFR mutations, with IC₅₀ values ranging from 3.5 nM to 108.3 nM^[1].
Lazertinib (10 nM (YUO-139 PDOs); 100 nM (YU-1092 PDCs); 72 h) upregulates EGFR expression on the surface of EGFR^G719S-mutant YUO-139 patient-derived organoids and EGFR^L861Q-mutant YU-1092 patient-derived cells after 72 h of treatment^[1].
Lazertinib (0.001-10 μM; 72 h) inhibits the viability of EGFR-mutant non-small cell lung cancer (NSCLC) cell lines after 72 h of incubation^[2].
Lazertinib (0.01-3.0 μM; 7 d, medium changed every 72 h) inhibits the long-term proliferation of PC-9 EGFR-mutant NSCLC cells in a concentration-dependent manner within 7 days, but fails to achieve complete growth inhibition at the tested concentrations^[2].
Lazertinib (100 nM; 4 h; 72 h) inhibits the phosphorylation of EGFR, ERK and AKT in PC-9 and HCC4011 EGFR-mutant NSCLC cells, but its inhibitory effects on ERK and AKT disappear by 72 h^[2].
Lazertinib (100 nM; 48 h) upregulates the expression of the anti-apoptotic protein MCL-1 in PC-9, HCC4011 and H1975 EGFR-mutant non-small cell lung cancer cells^[2].
Lazertinib (100 μM; 72 h) exhibits equivalent cytotoxicity in drug-sensitive parental cancer cell lines (HepG2, KB, S1, HEK293/Vector) and their multidrug-resistant (MDR) sublines with overexpressed ABCB1 or ABCG2. It reduces the IC₅₀ values of Vincristine (HY-N0488A), Doxorubicin (HY-15142A), Mitoxantrone (HY-13502), and Topotecan (HY-13768), respectively, but shows no significant effect on Cisplatin (HY-17394)^[3].
Lazertinib (0.1-1 μM; 24 h) does not induce neurite fragmentation in primary cultured dorsal root ganglion (DRG) neurons from the L3, L4 and L5 segments of adult mice^[4].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3 cells expressing EGFR G719S, S768I, G719A/S768I, L861Q, G719S/S768I, and S768I/L858R uncommon mutations
Concentration:

0.1-1000 nM
Incubation Time:

3 d
Result:

Inhibited cell viability with an IC₅₀ of 3.5 nM in EGFR G719S Ba/F3 cells. Inhibited cell viability with an IC₅₀ of 108.3 nM in EGFR S768I Ba/F3 cells. Inhibited cell viability with an IC₅₀ of 36.8 nM in EGFR G719A/S768I Ba/F3 cells. Inhibited cell viability with an IC₅₀ of 13.9 nM in EGFR L861Q Ba/F3 cells. Inhibited cell viability with an IC₅₀ of 21.9 nM in EGFR G719S/S768I Ba/F3 cells. Inhibited cell viability with an IC₅₀ of 7.2 nM in EGFR S768I/L858R Ba/F3 cells.

Cell Viability Assay^[2]

Cell Line:

PC-9, HCC4011, H1975, PC-9GXR, KPP-03, HCC827, HCC4006 (EGFR-mutant non-small cell lung cancer cell lines)
Concentration:

0.001-10 μM
Incubation Time:

72 h
Result:

Inhibited cell viability in all seven cell lines, with IC₅₀ values: PC-9: 0.103 μM; HCC4011: 0.161 μM; H1975: 4.074 μM; PC-9GXR: 1.379 μM; KPP-03: >10.0 μM; HCC827: <0.001 μM; HCC4006: 0.002 μM. Showed highest sensitivity in HCC827 and HCC4006, and lowest sensitivity in KPP-03.

Cell Viability Assay^[3]

Cell Line:

ABCB1-overexpressing MDR cells (KBv200, HepG2/adr, HEK293/ABCB1), ABCG2-overexpressing MDR cells (S1-MI-80, HEK293/ABCG2), and their parental sensitive cells
Concentration:

0.0625-0.25 μM
Incubation Time:

3 d
Result:

Reduced the IC₅₀ of vincristine (HY-N0488A) by up to 25.21-fold, doxorubicin (HY-15142A) by up to 14.82-fold, and paclitaxel by up to 15.90-fold in ABCB1-overexpressing cells. Reduced the IC₅₀ of mitoxantrone (HY-13502) by up to 8.97-fold and topotecan (HY-13768) by up to 11.94-fold in ABCG2-overexpressing cells. Did not significantly alter the IC₅₀ values of substrate drugs in parental sensitive cells, or the IC₅₀ of non-substrate cisplatin (HY-17394) in either sensitive or MDR cells.

In Vivo

Lazertinib (10 mg/kg; p.o.; once daily; days 27-29) achieves 26.3% and 141% tumor growth inhibition in Ba/F3 EGFR^G719S and YUO-139 EGFR^G719S xenograft models of non-small cell lung cancer, respectively^[1].
Mesylate of Lazertinib (10 mg/kg; p.o.; once daily; for 19 consecutive days) fails to inhibit tumor growth in the gefitinib (HY-50895)-resistant non-small cell lung cancer EGFR^L861Q YU-1092 xenograft model^[1].
Mesylate of Lazertinib (10 mg/kg; p.o.; once daily; administered until day 29) induces initial tumor regression but fails to achieve durable control in the EGFR-TKI-resistant non-small cell lung cancer YHIM-1008 EGFR^G719C/S768I xenograft model^[1].
Mesylate of Lazertinib (3 mg/kg; daily; for 31 consecutive days) exerts transient anti-tumor activity in PC-9 CDX tumors, with the tumors exhibiting regrowth within 3 weeks after the initiation of treatment^[2].
Mesylate of Lazertinib (10 mg/kg; p.o.; once every 3 days; 6 doses total) fails to inhibit the growth of ABCB1-overexpressing HepG2/adr xenografts. However, when combined with Doxorubicin (HY-15142A), it effectively reverses ABCB1-mediated multidrug resistance, significantly reduces tumor volume and weight, with no observed toxicity^[3].
Mesylate of Lazertinib (1 mM, 20 μL; plantar injection; single administration) induces TRPA1-dependent pain-like behavior in male C57BL/6J mice, with an average licking and biting duration of 58.91 seconds within 15 minutes^[4].

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

Animal Model:

nu/nu mice (6-week-old female)^[1]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 29 days
Result:

Induced a 141% tumor growth inhibition (TGI). Showed less durable responses than the lazertinib-amivantamab combination, with tumor regrowth observed in a subset of treated mice after treatment discontinuation.

Animal Model:

Athymic nude mice (4-6 weeks old, 16-20 g, subcutaneous inoculation with ABCB1-overexpressing HepG2/adr cells)^[3]
Dosage:

10 mg/kg (monotherapy); 10 mg/kg (combination with doxorubicin)
Administration:

p.o.; q3d; 6 doses
Result:

Did not reduce tumor volume or weight relative to saline control (monotherapy). Produced a remarkable decrease in tumor volume and tumor weight relative to saline group and doxorubicin-alone group (combination with doxorubicin). Showed no obvious changes in mouse body weight, indicating good tolerability (monotherapy and combination groups).

Animal Model:

C57BL/6J mice (5- to 6-week-old, male)^[4]
Dosage:

1 mM, 20 μL
Administration:

intraplantar; single dose
Result:

Increased average licking/biting time to 58.91 seconds over 15 minutes, compared to 6.832 seconds in vehicle-treated mice. Reduced total licking/biting time to 46.11 seconds when preinjected with TRPA1 antagonist HC-030031, compared to 105.6 seconds in vehicle-preinjected group.

Ensayo clínico

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

Chemical Information

No. CAS 1903008-80-9
Appearance Solid
Peso molecular 554.64
Fòrmula C₃₀H₃₄N₈O₃
Color Light yellow to yellow
SMILES

C=CC(NC1=CC(NC2=NC=CC(N3N=C(C4=CC=CC=C4)C(CN(C)C)=C3)=N2)=C(OC)C=C1N5CCOCC5)=O
Synonyms

YH25448; GNS-1480
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

Publications (3)

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Cancer Res

Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]

2025 Nov 6. PMID: 41196054
Drug Discov Ther

Solid phase extraction and high-performance liquid chromatographic determination of lazertinib in human plasma. [Abstract]

2025 Oct 17. PMID: 41110965
Patent

US20220177473A1.

Solvente y solubilidad

In Vitro:

DMSO : 3.33 mg/mL (6.00 mM; ultrasonic and warming and heat to 60°C; 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

1.8030 mL

9.0149 mL

18.0297 mL

5 mM

0.3606 mL

1.8030 mL

3.6059 mL

10 mM

---

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.

Calculadora de molaridad

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

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

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Volume _(start) Volume _(start)

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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: ≥ 0.9 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.9 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.9 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.9 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (9.0 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: ≥ 0.9 mg/mL (1.62 mM); Clear solution

This protocol yields a clear solution of ≥ 0.9 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 (9.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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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.

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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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

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Referencias

[1]. Oh SY, et al. The potential of lazertinib and amivantamab combination therapy as a treatment strategy for uncommon EGFR-mutated NSCLC. Cell Rep Med. 2025;6(2):101929. [Content Brief]

[2]. Matsui Y, et al. Initial AXL and MCL-1 inhibition contributes to abolishing lazertinib tolerance in EGFR-mutant lung cancer cells. Cancer Sci. 2024;115(10):3333-3345. [Content Brief]

[3]. Fan Y, et al. Lazertinib improves the efficacy of chemotherapeutic drugs in ABCB1 or ABCG2 overexpression cancer cells in vitro, in vivo, and ex vivo[J]. Molecular Therapy-Oncolytics, 2022, 24: 636-649.

[4]. Kim H, et al. EGFR Tyrosine Kinase Inhibitor Lazertinib Activates a Subset of Mouse Sensory Neurons Via TRPA1. J Pain. 2024;25(5):104435. [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, 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	1.8030 mL	9.0149 mL	18.0297 mL	45.0743 mL
DMSO	5 mM	0.3606 mL	1.8030 mL	3.6059 mL	9.0149 mL

Lazertinib

3 Cited Publications

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