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

China 248 India 1 United States 14 Global 263

MedChemexpress LLC

Tel: 021-58955995
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Musechem

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TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
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InvivoChem

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Fax: 708-557-7486
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Cckinase, Inc.

Tel: +1 (732)236-3202
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BOC Sciences

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Aladdin Scientific

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TargetMol Chemicals Inc.

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ApexBio Technology

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BOC Sciences

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Cayman Chemical Company

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United States Biological

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Combi-Blocks Inc.

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Matrix Scientific

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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:

Canagliflozin AZD-4547 Alectinib WZ4002 lenvatinib Mesylate Lenvatinib BKM-120 Olmutinib XL-647 Genistein AG 1478 HYDROCHLORIDE OSI-420 Anlotinib EGF816 Tucatinib Neratinib Poziotinib (HM781-36B) CO-1686

AZD 3759

AZD3759

AZD-3759

(2R)-2,4-Dimethyl-1-piperazinecarboxylic acid 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester

HY-18750

azd3579

1-Piperazinecarboxylic acid, 2,4-dimethyl-, 4-[(3-chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl ester, (2R)-

1-PIPERAZINECARBOXYLIC ACID, 2,4-DIMETHYL-, 4-[(3-CHLORO-2-FLUOROPHENYL)AMINO]-7-METHOXY-6-QUINAZOLINYL ESTER

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

zorifertinibum

AZD3759; AZD-3759; AZD 3759; ZORIFERTINIBUM; ZORIFERTINIB.

zorifertinib.

4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl 1-piperazinecarboxylic acid 2,4-dimethyl ester

4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (2R)-2,4-dimethylpiperazine-1-carboxylate

CS-1596

AZD-3759;AZD 3759;;AZD3759

AZD37591

4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl (R)-2,4-dimethylpiperazine-1-carboxylate

High Purity Azd 3759 CAS:

High Purity Azd3759/Azd-3759 CAS 1626387-80-1 with Steady Supply

Anti Cancer Azd3759, High Purity

AZD3759 Powder

Zorifertinib (AZD3759

TIANFU CHEM---AZD 3759

4-[(3-Chloro-2-fluorophenyl)amino]-7-methoxy-6-quinazolinyl (2R)-2,4-dimethyl-1-piperazinecarboxylate

AZD3759 AZD-3759

Mobotinib TAK788

(R)-4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate , AZD3759

Zolitinib

Zolitinib AZD3759

1626387-80-1

626387-80-1

C22H23ClFN5O3

API