Selective EGFR inhibitor
ChemicalBook > CAS DataBase List > AZD 3759

AZD 3759

Selective EGFR inhibitor
AZD 3759 Structure
AZD 3759
  • CAS No.1626387-80-1
  • Chemical Name:AZD 3759
  • CBNumber:CB53041786
  • Molecular Formula:C22H23ClFN5O3
  • Formula Weight:459.9
  • MOL File:1626387-80-1.mol
AZD 3759 Property
  • 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
  • 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
  • FDA UNII 67SX9H68W2
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

AZD 3759 Chemical Properties,Usage,Production

  • 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.

  • 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.
  • Uses AZD 3759 is EGFR inhibitor. It is a potent, oral active, central nervous system-penetrant, epidermal growth factor receptor tyrosine kinase inhibitor.
  • Biological Activity AZD3759 is a new, potent, oral, active central nervous system (CNS)‐penetrant EGFR inhibitor. It is mainly designed to effectively bypass the blood-brain barrier to address CNS metastasis in NSCLC patients carrying EGFR mutations, such as brain metastasis (BM) and dura mater (or pia mater, leptomeningeal metastases). AZD3759 is currently at a phase I/II research and development stage. At Km ATP concentrations, the half maximal inhibitory concentrations (IC50) were 0.3, 0.2, and 0.2 nM for wild‐type EGFR and mutated variants L858R and exon19Del, respectively. AZD3759 exhibited inhibitory effects on the proliferation of the phosphorylated (p) EGFR pathway and EGFR mutant-derived PC‐9 and H3255 cells, with IC50 of 7.7 nm and 7 nm, respectively. However, it had no inhibitory effect on the proliferation rate of H838 cells[4].
  • References [1] 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.
    [2] 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.
    [3] 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.
    [4] Qingjun Wu. “Determination and pharmacokinetic study of AZD-3759 in rat plasma by ultra performance liquid chromatography with triple quadrupole mass spectrometer.” Thoracic Cancer 9 11 (2018): 1383–1389.
AZD 3759 Preparation Products And Raw materials
Raw materials
Preparation Products
AZD 3759 Suppliers
Global(273)Suppliers
  • Supplier：
    AFINE CHEMICALS LIMITED
  • Tel：+86-0571-85134551
  • Email：sales@afinechem.com
  • Country：China
  • ProdList：15349
  • Advantage：58
  • Supplier：
    Henan Tianfu Chemical Co.,Ltd.
  • Tel：+86-0371-55170693<br/>+86-19937530512
  • Email：info@tianfuchem.com
  • Country：China
  • ProdList：21628
  • Advantage：55
  • Supplier：
    career henan chemical co
  • Tel：+86-0371-86658258<br/>+8613203830695
  • Email：sales@coreychem.com
  • Country：China
  • ProdList：29859
  • Advantage：58

Related articles

AZD 3759 Spectrum
1626387-80-1, AZD 3759Related Search:
  • API
  • 抑制剂
  • 合成有机化合物配体
  • 实验室
  • 化学试剂
  • 柏锦生物
  • 日用化学品
  • 原料
  • 标准品
  • 小分子
  • 染料
  • 细胞生物学试剂
  • 医药类-原料药
  • 科研原药系列
  • 原料药
  • 抗肿瘤类
  • 医药原料
  • 医药原料药
  • 小分子抑制剂
  • 原料药【仅供科研】
  • C22H23ClFN5O3
  • 626387-80-1
  • 化合物AZD3759,10 MM DMSO 溶液
  • PERFEMIKER]AZD3759,99%
  • 佐利替尼AZD3759
  • AZD3759佐利替尼
  • 佐利替尼
  • AZD375
  • 化合物AZD3759
  • (R)-4-((3-氯-2-氟苯基)氨基)-7-甲氧基喹唑啉-6-基 2,4-二甲基哌嗪-1-羧酸酯
  • AZD3759奥西替尼
  • EGFR抑制剂(AZD3759)
  • 奥希替尼9291,AZD3759
  • AZD3759奥希替尼
  • (2R)-2,4-二甲基-1-哌嗪羧酸 4-[(3-氯-2-氟苯基)氨基]-7-甲氧基-6-喹唑啉基酯
  • 1626387-80-1
  • Zorifertinib, 10 mM in DMSO
  • Zolitinib AZD3759
  • Zolitinib
  • (R)-4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate , AZD3759
  • Mobotinib TAK788
  • AZD3759 AZD-3759
  • 4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl (2R)-2,4-dimethyl-1-piperazinecarboxylate
  • TIANFU CHEM---AZD 3759
  • Zorifertinib (AZD3759
  • AZD3759 Powder
  • Anti Cancer Azd3759, High Purity
  • High Purity Azd3759/Azd-3759 CAS 1626387-80-1 with Steady Supply
  • High Purity Azd 3759 CAS:
  • 4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (R)-2,4-dimethylpiperazine-1-carboxylate
  • AZD37591
  • AZD-3759;AZD 3759;;AZD3759
  • CS-1596
  • 4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate
  • 4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl 1-piperazinecarboxylic acid 2,4-dimethyl ester
  • zorifertinib.
  • AZD3759; AZD-3759; AZD 3759; ZORIFERTINIBUM; ZORIFERTINIB.
  • zorifertinibum

Home

My