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AZD3759

Cat. No. M5164
AZD3759 Structure
Size Price Availability Quantity
5mg USD 80 In stock
10mg USD 120 In stock
50mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD3759 inhibits EGFR phosphorylation with IC50 of 7.2 nM in H3255 (L858R) cells. AZD3759 demonstrates inhibitory effects on both the pEGFR pathway and cell proliferation of EGFR mutation-derived cells PC-9 and H3255 with IC50 of 7.7 nM and 7 nM, respectively. In a brain metastasis PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) causes significant dose-dependent antitumor efficacy. AZD3759 shows good oral bioavailability in dogs, and penetrates extensively into monkey brain.

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 459.9
Formula C22H23ClFN5O3
CAS Number 1626387-80-1
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
Zeng Q, et al. J Med Chem. 2015 Oct 22;58(20):8200-15. PMID: 26313252.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD3759 supplier, EGFR/HER2, inhibitors

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