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AZD3759 hydrochloride

Cat. No. M10472
AZD3759 hydrochloride Structure
Synonym:

AZD-3759 HCl

Size Price Availability
10mg USD 110  USD110 4-7 Days
50mg USD 330  USD330 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD3759 hydrochloride is an orally available inhibitor of the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. AZD3759 also inhibits pEGFR in H838wt (IC50: 64.5 nM), H3255L858R (IC50: 7.2 nM), and PC-9exon 19Del (IC50: 7.4 nM), respectively. In cellular phosphorylation studies, AZD3759 also shows 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines.

In vivo, AZD3759 (7.5/15 mg/kg) can markedly decrease tumor area. In addition, modulation of pEGFR is detected by a single dose of AZD3759 at 15 mg/kg 1h after dosing.

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 496.36
Formula C22H24Cl2FN5O3
CAS Number 1626387-81-2
Purity >99%
Solubility DMSO ≥ 10 mg/mL
Storage at -20°C
References

[1] Chee-Seng Tan, et al. Lung Cancer. Next-generation epidermal growth factor receptor tyrosine kinase inhibitors in epidermal growth factor receptor -mutant non-small cell lung cancer

[2] Qingbei Zeng, et al. J Med Chem. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor

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Keywords: AZD3759 hydrochloride, AZD-3759 HCl supplier, EGFR/HER2, inhibitors

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