2. Membrane Transporter/Ion Channel Neuronal Signaling Protein Tyrosine Kinase/RTK JAK/STAT Signaling PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway Apoptosis
  3. TRP Channel EGFR Akt ERK Apoptosis
  4. Lazertinib mesylate

Lazertinib mesylate  (Synonyms: YH25448 mesylate; GNS-1480 mesylate)

Cat. No.: HY-109061B Purity: 99.85%
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Lazertinib (YH25448; GNS-1480) mesylate 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 mesylate 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 mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate 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 mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.

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Lazertinib mesylate

Lazertinib mesylate Chemical Structure

CAS No. : 2247995-37-3

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Based on 3 publication(s) in Google Scholar

Other Forms of Lazertinib mesylate:

Lazertinib mesylate Related Antibodies

Top Publications Citing Use of Products

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TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

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Description

Lazertinib (YH25448; GNS-1480) mesylate 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 mesylate 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 mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate 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 mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia[1][2][3][4].

IC50 & Target

EGFRT790M

 

TRPA1

 

In Vitro

Lazertinib mesylate (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 mesylate (10 nM (YUO-139 PDOs); 100 nM (YU-1092 PDCs); 72 h) upregulates EGFR expression on the surface of EGFRG719S-mutant YUO-139 patient-derived organoids and EGFRL861Q-mutant YU-1092 patient-derived cells after 72 h of treatment[1].
Lazertinib mesylate (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 mesylate (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 mesylate (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 mesylate (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 mesylate (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 mesylate (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.

Lazertinib mesylate Related Antibodies

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 days
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 Cytotoxicity 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: 72 h
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 mesylate (10 mg/kg; p.o.; once daily; days 27-29) achieves 26.3% and 141% tumor growth inhibition in Ba/F3 EGFRG719S and YUO-139 EGFRG719S 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 EGFRL861Q 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 EGFRG719C/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 (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 (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.
Molecular Weight

650.75

Formula

C31H38N8O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (153.67 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 1.5367 mL 7.6834 mL 15.3669 mL
5 mM 0.3073 mL 1.5367 mL 3.0734 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 1.5367 mL 7.6834 mL 15.3669 mL 38.4172 mL
5 mM 0.3073 mL 1.5367 mL 3.0734 mL 7.6834 mL
10 mM 0.1537 mL 0.7683 mL 1.5367 mL 3.8417 mL
15 mM 0.1024 mL 0.5122 mL 1.0245 mL 2.5611 mL
20 mM 0.0768 mL 0.3842 mL 0.7683 mL 1.9209 mL
25 mM 0.0615 mL 0.3073 mL 0.6147 mL 1.5367 mL
30 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2806 mL
40 mM 0.0384 mL 0.1921 mL 0.3842 mL 0.9604 mL
50 mM 0.0307 mL 0.1537 mL 0.3073 mL 0.7683 mL
60 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6403 mL
80 mM 0.0192 mL 0.0960 mL 0.1921 mL 0.4802 mL
100 mM 0.0154 mL 0.0768 mL 0.1537 mL 0.3842 mL
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  • 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:

Lazertinib2247995-37-3YH25448GNS-1480YH 25448YH-25448GNS1480GNS 1480TRP ChannelEGFRAktERKApoptosisTransient receptor potential channelsEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesapoptosisAKTABCG2TRPA1multidrug resistancenon-small cell lung cancerDRG neuronABCB1Inhibitorinhibitorinhibit

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