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

Mobocertinib (Synonyms: TAK-788; AP32788)

Cat. No.: HY-135815 Purity: 98.45%
Handling Instructions

Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.

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

Mobocertinib Chemical Structure

Mobocertinib Chemical Structure

CAS No. : 1847461-43-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 150 In-stock
Estimated Time of Arrival: December 31
100 mg USD 250 In-stock
Estimated Time of Arrival: December 31
500 mg USD 950 In-stock
Estimated Time of Arrival: December 31
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Mobocertinib:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity[1][2].

IC50 & Target[1]

EGFR exon 20 insertion

 

HER2

 

EGFR (WT)

35 nM (IC50)

In Vitro

Mobocertinib (TAK-788) inhibits all 14 mutant variants of EGFR (IC50s=2.4-22 nM), and all 6 mutant variants of HER2 (IC50s=2.4-26 nM), more potently than it inhibited WT EGFR (IC50=35 nM), including all 8 variants with exon 20 activating insertions[1].

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

In Vivo

In mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion, or with engineered Ba/F3 cells containing a HER2 exon 20 activating insertion, once daily oral dosing of Mobocertinib induced regression of tumors at doses that were well tolerated (30-100 mg/kg)[1].

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

Clinical Trial
Molecular Weight

585.70

Formula

C₃₂H₃₉N₇O₄

CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
10 mM 0.1707 mL 0.8537 mL 1.7074 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 98.92%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MobocertinibTAK-788 AP32788TAK788TAK 788AP32788AP 32788AP-32788EGFREpidermal growth factor receptorErbB-1HER1mutationsexoninsertionscancernon-smallcelllungNSCLCInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Mobocertinib
Cat. No.:
HY-135815
Quantity:
MCE Japan Authorized Agent: