Mobocertinib (TAK788)

Catalog No.S6813 Batch:S681302

Technical Data

Formula	C₃₂H₃₉N₇O₄
Molecular Weight	585.70	CAS No.	1847461-43-1
Solubility (25°C)*	In vitro	DMSO	10 mg/mL (17.07 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.

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.

References

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

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.

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