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Avitinib (AC0010)

Cat. No. M10337
Avitinib (AC0010) Structure
Synonym:

Abivertinib; AC-0010

Size Price Availability Quantity
5mg USD 87  USD87 In stock
10mg USD 133  USD133 In stock
25mg USD 263  USD263 In stock
100mg USD 633  USD633 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Avitinib (Abivertinib; AC0010) is a third-generation irreversible EGFR tyrosine kinase inhibitor, with potential antineoplastic activity. Avitinib (Abivertinib; AC0010) inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. 

In vivo, AC0010 (500 mg/kg; oral) administration daily resulted in complete remission of tumors with EGFR active and T790M mutations for over 143 days with no weight loss in a xenografte model.

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 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.

Chemical Information
Molecular Weight 487.53
Formula C26H26FN7O2
CAS Number 1557267-42-1
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

[1] Shujuan Huang, et al. J Cancer. Apigenin and Abivertinib, a novel BTK inhibitor synergize to inhibit diffuse large B-cell lymphoma in vivo and vitro

[2] Shujuan Huang, et al. Cancer Lett. Abivertinib, a novel BTK inhibitor: Anti-Leukemia effects and synergistic efficacy with homoharringtonine in acute myeloid leukemia

[3] Hanping Wang, et al. Lung Cancer. Penetration of the blood-brain barrier by avitinib and its control of intra/extra-cranial disease in non-small cell lung cancer harboring the T790M mutation

[4] Xiao Xu, et al. Mol Cancer Ther. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients

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Keywords: Avitinib (AC0010), Abivertinib; AC-0010 supplier, EGFR/HER2, inhibitors

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