Selective EGFR inhibitor
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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
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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
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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.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
19931
Product name
AZD 3759
Purity
≥98%
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
19931
Product name
AZD 3759
Purity
≥98%
Packaging
5mg
Price
$100
Updated
2024/03/01
Cayman Chemical
Product number
19931
Product name
AZD 3759
Purity
≥98%
Packaging
10mg
Price
$184
Updated
2024/03/01
Cayman Chemical
Product number
19931
Product name
AZD 3759
Purity
≥98%
Packaging
25mg
Price
$343
Updated
2024/03/01
TRC
Product number
A808165
Product name
AZD3759
Packaging
25mg
Price
$170
Updated
2021/12/16
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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

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AZD 3759 Suppliers

Jinan Chuanbei Biotechnology Co., Ltd
Tel
18654547380; 15269175648
Fax
0531-67802093
Email
qingyan7590@163.com
Country
China
ProdList
22
Advantage
58
Houxu Chemical (Shandong) Co., Ltd
Tel
18295613325
Email
2026425403@qq.com
Country
China
ProdList
18
Advantage
58
Scinova Biotech(Guangzhou) Co., Ltd.
Tel
13268215580
Email
scinova_sales@163.com
Country
China
ProdList
7023
Advantage
58
Jinan Good Medical &Technology Ltd Co.,
Tel
+86-0086-531-55562571,18953105926 +86-13553167512
Email
935170726@qq.com
Country
China
ProdList
73
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
Tel
17702719238 17702719238
Email
sales@sun-shinechem.com
Country
China
ProdList
976
Advantage
64
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19172
Advantage
64
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696
Email
info@hanhongsci.com
Country
China
ProdList
42958
Advantage
64
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
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View Lastest Price from AZD 3759 manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
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
Hebei Yanxi Chemical Co., Ltd.
Product
AZD3759 1626387-80-1
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20tons
Release date
2023-10-09
Handan Tongyi New Material Technology Co., Ltd
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

1626387-80-1, AZD 3759Related Search:


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  • API