AZD 3759
Selective EGFR inhibitor- Product Name
- AZD 3759
- CAS No.
- 1626387-80-1
- Chemical Name
- AZD 3759
- Synonyms
- azd3579;AZD3759;CS-1596;AZD-3759;AZD 3759;HY-18750;AZD37591;Zolitinib;zorifertinib.;zorifertinibum
- 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
- InChI
- InChI=1S/C22H23ClFN5O3/c1-13-11-28(2)7-8-29(13)22(30)32-19-9-14-17(10-18(19)31-3)25-12-26-21(14)27-16-6-4-5-15(23)20(16)24/h4-6,9-10,12-13H,7-8,11H2,1-3H3,(H,25,26,27)/t13-/m1/s1
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 19931
- Product name
- AZD 3759
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $32
- Updated
- 2024/03/01
- Product number
- 19931
- Product name
- AZD 3759
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 19931
- Product name
- AZD 3759
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $184
- Updated
- 2024/03/01
- Product number
- 19931
- Product name
- AZD 3759
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $343
- Updated
- 2024/03/01
- Product number
- A808165
- Product name
- AZD3759
- Packaging
- 25mg
- Price
- $170
- Updated
- 2021/12/16
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
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View Lastest Price from AZD 3759 manufacturers
- Product
- AZD3759 1626387-80-1
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-08-02
- Product
- AZD3759 1626387-80-1
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 0.99
- Supply Ability
- 20tons
- Release date
- 2023-10-09
- Product
- AZD 3759 1626387-80-1
- Price
- US $100.00/ASSAYS
- Min. Order
- 1ASSAYS
- Purity
- 99.9%
- Supply Ability
- 800kgs/month
- Release date
- 2021-03-09