Home Protein Tyrosine Kinase EGFR inhibitor - HER2 inhibitor Mobocertinib (TAK788) For research use only.

Mobocertinib (TAK788)

Synonyms: AP32788

Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.

Mobocertinib (TAK788) Chemical Structure

Mobocertinib (TAK788) Chemical Structure

CAS No. 1847461-43-1

Purity & Quality Control

Mobocertinib (TAK788) Related Products

Signaling Pathway

EGFR Signaling Pathways

EGFR Signaling Pathway

Biological Activity

Description Mobocertinib (TAK788, AP32788), an investigational TKI, is a potent, selective preclinical inhibitor of epidermal growth factor receptor (EGFR) and HER2 mutations. Mobocertinib (TAK788) is an antineoplastic agent.
Targets
EGFR [1] HER2 [1]
In vitro
In vitro

Mobocertinib (TAK-788), a novel irreversible EGFR TKI, is specifically designed to potently inhibit oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib inhibits viability of various EGFRex20ins-driven cell lines more potently than approved EGFR TKIs.[1]
Cell Research Cell lines NSCLC cell lines, Ba/F3 cells, A431 Cells, HEK293 cells
Concentrations 0.0003 -1 µM
Incubation Time 30 min, 2 h, 6h, 7 days
Method

Cells are plated into 96-well plates and dosed with a nine-point, threefold dilution series of compounds and incubated for 7 days. Viability is measured using the CellTiter-Glo assay. Dose–response curves are generated and used to calculate IC50 values.
In Vivo
In vivo

Mobocertinib suppresses growth of EGFRex20ins mutant tumors through EGFR inhibition. Combination treatment with mobocertinib and cetuximab improves efficacy in a head and neck squamous cell carcinoma model (CTG-2130) with EGFRex20ins D770_N771insGL.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05863819 Withdrawn
Non-small Cell Lung Cancer (NSCLC)
Takeda
 March 30 2024 --
NCT04576208 Withdrawn
Non-Small Cell Lung Cancer (NSCLC)
Takeda
 November 30 2020 Phase 2
NCT04056468 Completed
Hepatic Impairment|Healthy Volunteers
Millennium Pharmaceuticals Inc.|Takeda
 October 9 2020 Phase 1
NCT04441255 Completed
Healthy Volunteers
Takeda
 July 1 2020 Phase 1
NCT04056455 Completed
Renal Impairment|Healthy Volunteers
Millennium Pharmaceuticals Inc.|Takeda
 March 4 2020 Phase 1
NCT04051827 Completed
Carcinoma Non-Small-Cell Lung|Lung Neoplasms
Millennium Pharmaceuticals Inc.|Takeda
 December 23 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 585.70 Formula

C32H39N7O4
CAS No. 1847461-43-1 SDF --
Smiles CC(C)OC(=O)C1=CN=C(N=C1C2=CN(C3=CC=CC=C32)C)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 9 mg/mL ( (15.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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

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