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: 1847461-43-1

Selleck's Mobocertinib (TAK788) has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.78%
99.78

Mobocertinib (TAK788) Related Products

Signaling Pathway

Choose Selective EGFR Inhibitors

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NCT05863819 Withdrawn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NCT04576208 Withdrawn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
NCT03928327 Completed
Healthy Volunteers
Millennium Pharmaceuticals Inc.|Takeda
May 2 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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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.

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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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