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  3. Mobocertinib

Mobocertinib  (Synonyms: TAK-788; AP32788)

Cat. No.: HY-135815 Purity: 99.60%
COA Handling Instructions

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.

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

Mobocertinib Chemical Structure

Mobocertinib Chemical Structure

CAS No. : 1847461-43-1

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Customer Review

Based on 7 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

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[1][2].

IC50 & Target[1]

EGFR (WT)

 

EGFR exon 20 insertion

 

HER2

 

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 20G776>VC), Ba/F3 (HER2 exon 20YVMA) 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 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells
Concentration: 0.01, 0.1 and 1 μM
Incubation Time: 6 h
Result: Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA 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-Foxn1nu 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
Molecular Weight

585.70

Formula

C32H39N7O4

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7074 mL 8.5368 mL 17.0736 mL
5 mM 0.3415 mL 1.7074 mL 3.4147 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.60%

References

Complete Stock Solution Preparation Table

* 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.

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
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Mobocertinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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