Free shipping on all orders over $ 500

Mobocertinib

Cat. No. M9535
Mobocertinib Structure
Synonym:

TAK-788; AP32788

Size Price Availability Quantity
10mg USD 45  USD45 In stock
25mg USD 88  USD88 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
BBT-207

BBT-207 is a reversible, mutant-specific EGFR inhibitor with antitumor activity.

VRN-11

VRN-11 is an EGFR C797S inhibitor.

TRX-221

TRX-221 is an EGFR C797S inhibitor.

TAS-3351

TAS-3351 is an EGFR C797S inhibitor.

Larotinib mesylate hydrate

Larotinib mesylate hydrate is a potent, broad-spectrum, orally active tyrosine kinase inhibitor (TKI) that primarily targets EGFR with an IC50 of 0.6 nM.

  Catalog
Abmole Inhibitor Catalog




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


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.