2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Mobocertinib succinate

Mobocertinib succinate  (Synonyms: TAK-788 succinate; AP32788 succinate)

Cat. No.: HY-135815A Purity: 99.61%
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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.

Mobocertinib succinate Chemical Structure

Mobocertinib succinate Chemical Structure

CAS No. : 2389149-74-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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5 mg USD 35 In-stock
10 mg USD 50 In-stock
25 mg USD 85 In-stock
50 mg USD 145 In-stock
100 mg USD 230 In-stock
500 mg USD 600 In-stock
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Based on 6 publication(s) in Google Scholar

Other Forms of Mobocertinib succinate:

Mobocertinib succinate Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target[1]

EGFR exon 20 insertion

 

HER2

 

EGFR (WT)

 

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 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.

Mobocertinib succinate Related Antibodies

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 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-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

703.78

Formula

C36H45N7O8
CAS No.
Appearance

Solid

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
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)

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4209 mL 7.1045 mL 14.2090 mL
5 mM 0.2842 mL 1.4209 mL 2.8418 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, 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.

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  • 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    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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • 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

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).

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

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: 99.61%

COA (263 KB) HNMR (172 KB) LCMS (120 KB)

Handling Instructions (2659 KB)
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, 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.

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
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Mobocertinib succinate 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.

Keywords:

Mobocertinib2389149-74-8TAK-788AP32788TAK788TAK 788AP 32788AP-32788EGFREpidermal growth factor receptorErbB-1HER1NSCLCEGFRex20insLU0387A431HCC827HCC4011H1975CUTO14Inhibitorinhibitorinhibit

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