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Mobocertinib (TAK788) EGFR inhibitor

Name: Mobocertinib (TAK788)
Brand: Selleck Chemicals
SKU: S6813
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S6813

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

Chemical Structure

Molecular Weight: 585.70

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Quality Control

Batch: Purity: 99.78%

99.78

Related Targets	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other EGFR Inhibitors	Sunvozertinib Icotinib Hydrochloride AG-490 AG-1478 Canertinib (CI-1033) Rociletinib (CO-1686) WZ4002 Genistein Poziotinib (NOV120101, HM781-36B) PD153035

Solubility

In vitro
Batch:

DMSO : 9 mg/mL (15.36 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Chemical Information, Storage & Stability

Molecular Weight	585.70	Formula	C₃₂H₃₉N₇O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1847461-43-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AP32788			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

Mechanism of Action

Targets/IC₅₀/Ki	EGFR HER2
In vitro	Specifically designed to potently inhibit oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR, Mobocertinib (TAK-788) is a novel irreversible EGFR TKI. It inhibits viability of various EGFRex20ins-driven cell lines more potently than approved EGFR TKIs.
In vivo	Mobocertinib (TAK788) suppresses growth of EGFRex20ins mutant tumors through EGFR inhibition. Combination treatment with this compound and cetuximab improves efficacy in a head and neck squamous cell carcinoma model (CTG-2130) with EGFRex20ins D770_N771insGL.
References	[1] https://pubmed.ncbi.nlm.nih.gov/33632773/ [2] https://patents.google.com/patent/WO2019222093A1

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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