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AZD3759

Catalog No.
B5962
具有口服活性的EGFR抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 880.00
现货
5mg
¥ 700.00
现货
10mg
¥ 1,000.00
现货
50mg
¥ 3,000.00
现货
100mg
¥ 4,500.00
现货

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Background

AZD3759 is a potent and oral active inhibitor of EGFR (IC50= 7.0-7.7 nM) with antineoplastic activity.

EGFR (epidermal growth factor receptor) is a cell-surface receptor tyrosine kinase. The receptor activation leads to dimerization and tyrosine autophosphorylation. It induces a cascade of downstream cellular responses such as modification in gene expression, cell proliferation and cytoskeletal rearrangement etc.

AZD3759 shows equally potent inhibitory effect on cell phosphorylation or proliferation in EGFR-activating mutant cell lines (PC-9 and H3255) in the range of 7.0−7.7nM. In cellular phosphorylation assays, AZD3759 also exhibits 9-fold inhibition selectivity in EGFR-activating

mutant cell lines over EGFR wild-type cell lines (H838). [1]

In brain metastasis mouse model, AZD3759 demonstrates prominent antitumor efficacy in a dose dependent manner (∼78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively, 4 weeks after treatment, with <20% body weight loss). In addition, at the doses of 7.5 and 15 mg/k, AZD3759 significantly decreases tumor area in the brain tissue collected from the same mouse model. [1]

Reference:
Zeng Q, Wang J, Cheng Z et al.  Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt459.90
Cas No.1626387-80-1
FormulaC22H23ClFN5O3
Solubility≥23mg/mL in DMSO
Chemical Name(R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate
SDFDownload SDF
Canonical SMILESClC1=CC=CC(NC2=NC=NC3=CC(OC)=C(OC(N4[C@H](C)CN(C)CC4)=O)C=C23)=C1F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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