Free shipping on all orders over $ 500

Mobocertinib

Cat. No. M9535
Mobocertinib Structure
Synonym:

TAK-788; AP32788

Size Price Availability Quantity
10mg USD 60  USD60 In stock
25mg USD 90  USD90 In stock
50mg USD 150  USD150 In stock
100mg USD 250  USD250 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Mobocertinib (TAK-788) is an investigational TKI with potent, selective preclinical activity against activating EGFR and HER2 mutations, including exon 20 insertions. 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). Daily oral dosing of Mobocertinib in mice implanted with a patient-derived tumor containing an EGFR exon 20 activating insertion induced regression of tumors at doses that were well tolerated (30-100 mg/kg).

*This compound is unstable in solutions, freshly prepared is recommended.

Chemical Information
Molecular Weight 585.70
Formula C32H39N7O4
CAS Number 1847461-43-1
Solubility (25°C) DMSO ≥ 8 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ashiq Masood, et al. Semin Oncol. Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations: Focus on Afatinib.

Related EGFR/HER2 Products
Necitumumab

Necitumumab is a second-generation fully humanized immunoglobulin G1 (IgG1), epidermal growth factor (EGFR) receptor monoclonal antibody that specifically blocks the ligand binding site of EGFR.

Imgatuzumab

Imgatuzumab (RG 7160) is a humanized monoclonal antibody against the EGFR. Imgatuzumab acts as an immunomodulator. Imgatuzumab can be used in research of cancer.

Intetumumab

Intetumumab (CNTO 95) is a potent anti-EGFR monoclonal antibody that is glycoengineered for enhanced antibody-dependent cellular cytotoxicity (ADCC). Intetumumab can be used in research of cancer.

Zalutumumab

Zalutumumab is a high affinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer.

Izalontamab

Izalontamab (SI-B001) is a bispecific anti-EGFR/HER3 monoclonal antibody with high selectivity for EGFR/HER3 heterodimer. Izalontamab can be used for the research of cancer.

  Catalog
Abmole Inhibitor Catalog




Keywords: Mobocertinib, TAK-788; AP32788 supplier, EGFR/HER2, inhibitors, activators

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.