Supplier Related Products Identification Chemical Properties Questions and Answers (Q&A) Questions And Answer
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1626387-80-1

Supplier Related Products Identification Chemical Properties Questions and Answers (Q&A) Questions And Answer

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Identification

Name
AZD 3759
CAS
1626387-80-1
Synonyms
AZD3759
azd3579
AZD-3759
AZD 3759
HY-18750
4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carb
(R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate
(2R)-2,4-Dimethyl-1-piperazinecarboxylic acid 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester
1-Piperazinecarboxylic acid, 2,4-dimethyl-, 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester, (2R)-
EINECS(EC#)
1592732-453-0
Molecular Formula
C22H23ClFN5O3
MDL Number
MFCD29058564
MOL File
1626387-80-1.mol
Molecular Weight
459.91

Chemical Properties

Boiling point 
571.4±50.0 °C(Predicted)
density 
1.358±0.06 g/cm3(Predicted)
pka
6.71±0.40(Predicted)

Questions and Answers (Q&A)

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. 
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.

Questions And Answer

Selective EGFR inhibitor

AZD3759 is a selective EGFR inhibitor that can fully penetrate the blood-brain barrier (BBB), with equal free concentrations in the blood, cerebrospinal fluid, and brain tissue. Treatment with AZD3759 causes tumor regression in subcutaneous xenograft, leptomeningeal metastasis (LM), and brain metastasis (BM) lung cancer models and prevents the development of BM in nude mice.


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