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HomeProduct name listAZD 3759

AZD 3759

  • CAS NO.:1626387-80-1
  • Empirical Formula: C22H23ClFN5O3
  • Molecular Weight: 459.9
  • MDL number: MFCD29058564
  • EINECS: 1592732-453-0
  • SAFETY DATA SHEET (SDS)
  • Update Date: 2024-11-19 20:33:22
AZD 3759 Structural

What is AZD 3759?

Description

AZD3759 is an EGFP inhibitor (Epidermal growth factor receptor tyrosine kinase inhibitor) with blood brain barrier (BBB) penetration. It has the potential for the treatment of non-small cell lung cancer (NSCLC), with brain metastases (BM) and leptomengingeal metastases (LM) since this type of cancer often contain a lot of activating mutations of the epidermal growth factor receptor (EGFR). It has excellent capability of penetrating the blood brain barrier to reach the central nervous system.

The Uses of AZD 3759

AZD 3759 is EGFR inhibitor. It is a potent, oral active, central nervous system-penetrant, epidermal growth factor receptor tyrosine kinase inhibitor.

References

Zeng, Qingbei, et al. "Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR TKI)." Journal of Medicinal Chemistry 58.20(2015):8200.
Yang, Zhenfan, et al. "Abstract LB-217: Antitumor activities of AZD3759, a novel EGFR inhibitor with excellent penetration across central nervous system (CNS), in preclinical animal models." Cancer Research 76.14 Supplement(2016):LB-217-LB-217.
Xiong, S., et al. "Determination of AZD3759 in rat plasma and brain tissue by LC-MS/MS and its application in pharmacokinetic and brain distribution studies." Journal of Pharmaceutical & Biomedical Analysis140(2017):362-366.

Properties of AZD 3759

Boiling point: 571.4±50.0 °C(Predicted)
Density  1.358±0.06 g/cm3(Predicted)
storage temp.  Store at -20°C
solubility  ≥23 mg/mL in DMSO; insoluble in H2O; ≥8.32 mg/mL in EtOH with ultrasonic
form  solid
pka 6.71±0.40(Predicted)
color  White to off-white

Safety information for AZD 3759

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for AZD 3759

InChIKey MXDSJQHFFDGFDK-CYBMUJFWSA-N
SMILES N1(C(OC2C(OC)=CC3C(C=2)=C(NC2=CC=CC(Cl)=C2F)N=CN=3)=O)CCN(C)C[C@H]1C

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