Mobocertinib (TAK788)

Catalog No.S6813 Batch:S681301

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Technical Data

Formula

C32H39N7O4

Molecular Weight 585.70 CAS No. 1847461-43-1
Solubility (25°C)* In vitro DMSO 9 mg/mL (15.36 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

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.

Protocol (from reference)

Cell Assay:

[1]

  • 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.

Selleck's Mobocertinib (TAK788) has been cited by 3 publications

Mobocertinib in Patients with EGFR Exon 20 Insertion-Positive Non-Small Cell Lung Cancer (MOON): An International Real-World Safety and Efficacy Analysis [ Int J Mol Sci, 2024, 25(7)3992] PubMed: 38612799
Secondary Mutations of the EGFR Gene That Confer Resistance to Mobocertinib in EGFR Exon 20 Insertion [ J Thorac Oncol, 2023, S1556-0864(23)00797-9] PubMed: 37666482
Extensive functional evaluation of exon 20 insertion mutations of EGFR [ Lung Cancer, 2020, 152:135-142] PubMed: 33395611

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.