Art. -Nr.: HY-135815

Mobocertinib

(Synonyms: TAK-788; AP32788)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

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

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Reinheit: 99.60%
CAS. Nr.: 1847461-43-1
Formel: C₃₂H₃₉N₇O₄
Molecular Weight:585.70

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Mobocertinib Chemical Structure

CAS. Nr.: 1847461-43-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR (WT)

EGFR exon 20 insertion

HER2

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	EC₅₀	1676 nM Compound: 2	Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
A-431	GI₅₀	26 nM Compound: TAK-788	Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against human A-431 cells harboring wildtype EGFR assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	EC₅₀	1.1 nM Compound: 2	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	EC₅₀	2711 nM Compound: 2	Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay	[PMID: 37197473]
BaF3	GI₅₀	9 nM Compound: TAK-788	Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771ins_SVD mutant assessed as cell growth inhibition incubated for 72 hrs by CellTiter Glo assay	[PMID: 37406381]
BaF3	IC₅₀	1.9 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	10.1 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1062.9 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	1133.7 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	2168.1 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	27.1 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	34.5 nM Compound: TAK-788	Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	3814.5 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	3946 nM Compound: 21c; TAK-788	Anticancer activity against parental mouse BaF3 cells assessed as cell viability incubated for 3 days by Cell Titer-Glo assay Anticancer activity against parental mouse BaF3 cells assessed as cell viability incubated for 3 days by Cell Titer-Glo assay	[PMID: 36423823]
BaF3	IC₅₀	4.3 nM Compound: TAK-788	Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	47.6 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	5 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	8.3 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	8.9 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]
BaF3	IC₅₀	9 nM Compound: Mobocertinib	Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay	[PMID: 36384036]

In Vitro

Mobocertinib (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC₅₀ of 21 nM^[1].
Mobocertinib (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 (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells^[1].
Mobocertinib (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling^[1].
Mobocertinib (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 (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.

Chemical Information

CAS. Nr. 1847461-43-1
Appearance Solid
Molecular Weight 585.70
Formel C₃₂H₃₉N₇O₄
Color Off-white to light 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
Synonyms

TAK-788; AP32788
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

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
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
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
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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (42.68 mM; ultrasonic and warming and heat to 80°C; 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

1.7074 mL

8.5368 mL

17.0736 mL

5 mM

0.3415 mL

1.7074 mL

3.4147 mL

10 mM

0.1707 mL

0.8537 mL

1.7074 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 1.25 mg/mL (2.13 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC/saline water

Solubility: 25 mg/mL (42.68 mM); Suspended solution; Need ultrasonic

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[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]. Han 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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7074 mL	8.5368 mL	17.0736 mL	42.6840 mL
	5 mM	0.3415 mL	1.7074 mL	3.4147 mL	8.5368 mL
	10 mM	0.1707 mL	0.8537 mL	1.7074 mL	4.2684 mL
	15 mM	0.1138 mL	0.5691 mL	1.1382 mL	2.8456 mL
	20 mM	0.0854 mL	0.4268 mL	0.8537 mL	2.1342 mL
	25 mM	0.0683 mL	0.3415 mL	0.6829 mL	1.7074 mL
	30 mM	0.0569 mL	0.2846 mL	0.5691 mL	1.4228 mL
	40 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0671 mL

Mobocertinib

12 Cited Publications

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Mobocertinib

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Publications Citing Use of MedChemExpress (MCE) Mobocertinib

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Mobocertinib Related Classifications

HY-135815 Related Classifications