Mobocertinib mesylate
Based on 12 publication(s) in Google Scholar
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
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- CAS. Nr.: 2389149-85-1
- Formel: C33H43N7O7S
- Molecular Weight:681.80
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Mobocertinib mesylate
More- Cancer Res. 2025 Nov 6. [Abstract]
- Acta Pharm Sin B. 2023 Jun;13(6):2613-2627. [Abstract]
- Clin Cancer Res. 2025 Jun 4:OF1-OF17. [Abstract]
- Cells. 2021 Dec 17;10(12):3561. [Abstract]
- Lung Cancer. 2025 Apr:202:108479. [Abstract]
- Lung Cancer. 2023 Jul:181:107250. [Abstract]
- Toxicology. 2024 May 15:505:153830. [Abstract]
- Mol Pharm. 2022 Nov 7;19(11):4320-4332. [Abstract]
- JTO Clin Res Rep. 2023 Nov 27;5(1):100614. [Abstract]
- JTO Clin Res Rep. 2023 Jan 24;4(3):100462. [Abstract]
- Biochem Biophys Res Commun. 2025 Sep 16:780:152460. [Abstract]
- Biomed Chromatogr. 2025 Feb;39(2):e6063. [Abstract]
Alle EGFR Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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HER2 |
EGFR exon 20 insertion |
EGFR (WT) |
Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM[1].
Mobocertinib mesylate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))[1].
Mobocertinib mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib mesylate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LU0387 (NPH) cells
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Concentration:1.5 nM-10 μM
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Incubation Time:7 days
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Result:Showed good inhibition activity for LU0387 (NPH) cells with IC50 of 21 nM.
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Cell Line:A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
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Concentration:
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Incubation Time:2 h
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Result:Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC50s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC50 of 35 nM).
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Cell Line:CUTO14 (ASV) cells
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Concentration:0.1 nM-1 μM
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Incubation Time:6 h
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Result:Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.
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Cell Line:HCC827 (D), HCC4011 (L), H1975 (LT) cells
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Concentration:0.3 nM-1 μM
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Incubation Time:6 h
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Result:Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.
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Cell Line:H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells
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Concentration:0.01, 0.1 and 1 μM
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Incubation Time:6 h
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Result:Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Animal model: Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model)[1].
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Dosage:3, 10, 30 mg/kg
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Administration:Oral; once daily for 20 days.
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Result:Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.
Chemical Information
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CAS. Nr. 2389149-85-1
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Molecular Weight 681.80
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Formel C33H43N7O7S
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SMILES
O=C(C1=CN=C(NC2=CC(NC(C=C)=O)=C(N(CCN(C)C)C)C=C2OC)N=C1C3=CN(C)C4=C3C=CC=C4)OC(C)C.O=S(O)(C)=O
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Synonyms
TAK-788 mesylate; AP32788 mesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (12)
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Journal Impact Factor
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Most Recent
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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 -
Acta Pharm Sin B
Antitumor activity of aumolertinib, a third-generation EGFR tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon EGFR mutations. [Abstract]2023 Jun;13(6):2613-2627. PMID: 37425047 -
Clin Cancer Res
STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]2025 Jun 4:OF1-OF17. PMID: 40465424 -
Cells
EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios. [Abstract]2021 Dec 17;10(12):3561. PMID: 34944068 -
Lung Cancer
Efficacy of EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer with EGFR exon 19 insertions: clinical-genomic, preclinical analysis through LC-SCRUM-Asia (multi-institutional genomic screening registry). [Abstract]2025 Apr:202:108479. PMID: 40088581 -
Lung Cancer
EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors. [Abstract]2023 Jul:181:107250. PMID: 37196448 -
Toxicology
Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]2024 May 15:505:153830. PMID: 38754619 -
Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563 -
JTO Clin Res Rep
The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors. [Abstract]2023 Nov 27;5(1):100614. PMID: 38229766 -
JTO Clin Res Rep
The EGFR C797S Mutation Confers Resistance to a Novel EGFR Inhibitor CLN-081 to EGFR Exon 20 Insertion Mutations. [Abstract]2023 Jan 24;4(3):100462. PMID: 36915628 -
Biochem Biophys Res Commun
Electrophysiological consequences of acute mobocertinib exposure in isolated rat and guinea-pig hearts and transfected cell lines. [Abstract]2025 Sep 16:780:152460. PMID: 40818285 -
Biomed Chromatogr
A Simple and Sensitive LC-MS/MS Method for the Determination of Mobocertinib and Its Metabolite Desmethyl-Mobocertinib in Human Plasma and Its Application to Clinical Pharmacokinetic Study. [Abstract]2025 Feb;39(2):e6063. PMID: 39748454
Reinheit & Dokumentation
Verweise
[1]. Gonzalvez F, et al. Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687. [Content Brief]
[2]. Han H, et al. Targeting HER2 Exon 20 Insertion-Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib. Cancer Res. 2021 Oct 15;81(20):5311-5324. [Content Brief]
Calculators
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Mobocertinib mesylate Related Classifications
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