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Mobocertinib

Cat. No. M9535
Mobocertinib Structure
Synonym:

TAK-788; AP32788

Size Price Availability Quantity
10mg USD 410 In stock
25mg USD 790 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 585.70
Formula C32H39N7O4
CAS Number 1847461-43-1
Purity >98.5%
Solubility DMSO ≥ 8 mg/mL
Storage at -20°C
References

Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer Harboring Uncommon EGFR Mutations: Focus on Afatinib.
Ashiq Masood, et al. Semin Oncol. 2019 Jun;46(3):271-283. PMID: 31558282.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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