Choose Your Country or Region

Mobocertinib (TAK788)

Name: Mobocertinib (TAK788)
Brand: Selleck Chemicals
SKU: S6813
Rating: 5 (2 reviews)

Synonyms: AP32788

Catalog No.S6813 Purity: 99.78%

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

CAS: 1847461-43-1

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

Purity & Quality Control

Batch: Purity: 99.78%

99.78

Other EGFR Products

Related compound libraries

Choose Selective EGFR Inhibitors

Biological Activity

Description

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05863819	Withdrawn	Non-small Cell Lung Cancer (NSCLC)	Takeda	March 30 2024	--
NCT04576208	Withdrawn	Non-Small Cell Lung Cancer (NSCLC)	Takeda	November 30 2020	Phase 2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

References

Chemical lnformation & 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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):