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
- Molecular Weight:
- 459.9
- MOL File:
- 1626387-80-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/8/2 15:22:07
| 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 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
AZD 3759 Chemical Properties,Uses,Production
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.
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
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15372 | 58 | Inquiry |
| Shijiazhuang Tongyang Import and Export Co., LTD | 18031361688; | China | 987 | 58 | Inquiry |
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 | China | 5873 | 58 | Inquiry |
| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 +86-18600796368 | China | 375 | 58 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21662 | 55 | Inquiry |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | China | 9242 | 55 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32835 | 60 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29899 | 58 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
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