Cat. No.: HY-135815A

Mobocertinib succinate

(Synonyms: TAK-788 succinate; AP32788 succinate)

12 Cited Publications

Customer Review

Based on 12 publication(s) in Google Scholar

Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research.

For research use only. We do not sell to patients.

Purity: 99.83%
CAS No.: 2389149-74-8
Formula: C₃₆H₄₅N₇O₈
Molecular Weight:703.78

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Mobocertinib succinate Chemical Structure

CAS No.: 2389149-74-8

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (12)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR exon 20 insertion

HER2

EGFR (WT)

All EGFR Isoforms :

In Vitro

Mobocertinib succinate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC₅₀ of 21 nM^[1].
Mobocertinib succinate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))^[1].
Mobocertinib succinate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells^[1].
Mobocertinib succinate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling^[1].
Mobocertinib succinate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

LU0387 (NPH) cells
Concentration:

1.5 nM-10 μM
Incubation Time:

7 days
Result:

Showed good inhibition activity for LU0387 (NPH) cells with IC₅₀ of 21 nM.

Cell Viability Assay^[1]

Cell Line:

A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:
Incubation Time:

2 h
Result:

Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC₅₀s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC₅₀ of 35 nM).

Western Blot Analysis^[1]

Cell Line:

CUTO14 (ASV) cells
Concentration:

0.1 nM-1 μM
Incubation Time:

6 h
Result:

Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively.

Western Blot Analysis^[1]

Cell Line:

HCC827 (D), HCC4011 (L), H1975 (LT) cells
Concentration:

0.3 nM-1 μM
Incubation Time:

6 h
Result:

Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells.

Western Blot Analysis^[2]

Cell Line:

H1781 (HER2 Exon 20^G776>VC), Ba/F3 (HER2 exon 20^YVMA) cells
Concentration:

0.01, 0.1 and 1 μM
Incubation Time:

6 h
Result:

Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20^YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.

In Vivo

Mobocertinib succinate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female Athymic Nude-Foxn1^nu mice (human NSCLC H1975 LT tumor model)^[1].
Dosage:

3, 10, 30 mg/kg
Administration:

Oral; once daily for 20 days.
Result:

Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2389149-74-8
Appearance Solid
Molecular Weight 703.78
Formula C₃₆H₄₅N₇O₈
Color White to yellow
SMILES

O=C(C1=CN=C(NC2=CC(NC(C=C)=O)=C(N(CCN(C)C)C)C=C2OC)N=C1C3=CN(C)C4=C3C=CC=C4)OC(C)C.O=C(O)CCC(O)=O
Synonyms

TAK-788 succinate; AP32788 succinate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (12)

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Journal Impact Factor

Cancer Res

Enozertinib is a Selective, Brain-penetrant EGFR inhibitor for Treating Non-small Cell Lung Cancers with EGFR Exon 20 and Atypical Mutations. [Abstract]

2025 Nov 6. PMID: 41196054
Acta Pharm Sin B

Antitumor activity of aumolertinib, a third-generation EGFR tyrosine kinase inhibitor, in non-small-cell lung cancer harboring uncommon EGFR mutations. [Abstract]

2023 Jun;13(6):2613-2627. PMID: 37425047
Clin Cancer Res

STX-721, a Covalent EGFR/HER2 Exon 20 Inhibitor, Utilizes Exon 20-Mutant Dynamic Protein States and Achieves Unique Mutant Selectivity Across Human Cancer Models. [Abstract]

2025 Jun 4:OF1-OF17. PMID: 40465424
Cells

EGFR-D770>GY and Other Rare EGFR Exon 20 Insertion Mutations with a G770 Equivalence Are Sensitive to Dacomitinib or Afatinib and Responsive to EGFR Exon 20 Insertion Mutant-Active Inhibitors in Preclinical Models and Clinical Scenarios. [Abstract]

2021 Dec 17;10(12):3561. PMID: 34944068
Toxicology

Phosphoproteomics reveals a novel mechanism underlying the proarrhythmic effects of nilotinib, vandetanib, and mobocertinib. [Abstract]

2024 May 15:505:153830. PMID: 38754619
Mol Pharm

Machine Learning Models Identify New Inhibitors for Human OATP1B1. [Abstract]

2022 Nov 7;19(11):4320-4332. PMID: 36269563
Lung Cancer

Efficacy of EGFR tyrosine kinase inhibitors in patients with non-small cell lung cancer with EGFR exon 19 insertions: clinical-genomic, preclinical analysis through LC-SCRUM-Asia (multi-institutional genomic screening registry). [Abstract]

2025 Apr:202:108479. PMID: 40088581
Lung Cancer

EGFR exon 19 insertion EGFR-K745_E746insIPVAIK and others with rare XPVAIK amino-acid insertions: Preclinical and clinical characterization of the favorable therapeutic window to all classes of approved EGFR kinase inhibitors. [Abstract]

2023 Jul:181:107250. PMID: 37196448
JTO Clin Res Rep

The Impact of On-Target Resistance Mediated by EGFR-T790M or EGFR-C797S on EGFR Exon 20 Insertion Mutation Active Tyrosine Kinase Inhibitors. [Abstract]

2023 Nov 27;5(1):100614. PMID: 38229766
JTO Clin Res Rep

The EGFR C797S Mutation Confers Resistance to a Novel EGFR Inhibitor CLN-081 to EGFR Exon 20 Insertion Mutations. [Abstract]

2023 Jan 24;4(3):100462. PMID: 36915628
Biochem Biophys Res Commun

Electrophysiological consequences of acute mobocertinib exposure in isolated rat and guinea-pig hearts and transfected cell lines. [Abstract]

2025 Sep 16:780:152460. PMID: 40818285
Biomed Chromatogr

A Simple and Sensitive LC-MS/MS Method for the Determination of Mobocertinib and Its Metabolite Desmethyl-Mobocertinib in Human Plasma and Its Application to Clinical Pharmacokinetic Study. [Abstract]

2025 Feb;39(2):e6063. PMID: 39748454

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (177.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4209 mL

7.1045 mL

14.2090 mL

5 mM

0.2842 mL

1.4209 mL

2.8418 mL

10 mM

0.1421 mL

0.7104 mL

1.4209 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (289 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gonzalvez F, et al. Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer. Cancer Discov. 2021 Jul;11(7):1672-1687. [Content Brief]

[2]. an H, et al. Targeting HER2 Exon 20 Insertion-Mutant Lung Adenocarcinoma with a Novel Tyrosine Kinase Inhibitor Mobocertinib. Cancer Res. 2021 Oct 15;81(20):5311-5324. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.4209 mL	7.1045 mL	14.2090 mL	35.5225 mL
	5 mM	0.2842 mL	1.4209 mL	2.8418 mL	7.1045 mL
	10 mM	0.1421 mL	0.7104 mL	1.4209 mL	3.5522 mL
	15 mM	0.0947 mL	0.4736 mL	0.9473 mL	2.3682 mL
	20 mM	0.0710 mL	0.3552 mL	0.7104 mL	1.7761 mL
	25 mM	0.0568 mL	0.2842 mL	0.5684 mL	1.4209 mL
	30 mM	0.0474 mL	0.2368 mL	0.4736 mL	1.1841 mL
	40 mM	0.0355 mL	0.1776 mL	0.3552 mL	0.8881 mL
	50 mM	0.0284 mL	0.1421 mL	0.2842 mL	0.7104 mL
	60 mM	0.0237 mL	0.1184 mL	0.2368 mL	0.5920 mL
	80 mM	0.0178 mL	0.0888 mL	0.1776 mL	0.4440 mL
	100 mM	0.0142 mL	0.0710 mL	0.1421 mL	0.3552 mL

Mobocertinib succinate

12 Cited Publications

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Mobocertinib succinate

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Publications Citing Use of MedChemExpress (MCE) Mobocertinib succinate

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (12)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Mobocertinib succinate Related Classifications

Cat. No.: HY-135815A