AZD3759
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZD3759是一种强效的和口服有效的EGFR(IC50= 7.0-7.7 nM)抑制剂,具有抗肿瘤活性。
EGFR(表皮生长因子受体)是一种细胞表面受体酪氨酸激酶。受体活化导致二聚化和酪氨酸自磷酸化。其诱导下游细胞应答级联,如基因表达修饰、细胞增殖和细胞骨架重排等。
AZD3759在7.0-7.7 nM 范围内时对EGFR激活的突变细胞系(PC-9和H3255)的细胞磷酸化或增殖显示出同等强效的抑制作用。在细胞磷酸化试验中,AZD3759对EGFR激活的突变细胞系表现出优于EGFR野生型细胞系(H838)9倍的抑制选择性。[1]
在脑癌转移小鼠模型中,AZD3759表现出剂量依赖性的显著抗肿瘤功效(治疗4周后,7.5 mg/kg qd时约78%的肿瘤生长抑制,15 mg/kg qd时肿瘤消退,体重减轻小于20%)。此外,在7.5和15 mg/kg剂量时,AZD3759显著降低相同小鼠模型中收集的脑组织中的肿瘤面积。 [1]
参考文献:
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
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 459.90 |
Cas No. | 1626387-80-1 |
Formula | C22H23ClFN5O3 |
Solubility | ≥23 mg/mL in DMSO; insoluble in H2O; ≥8.32 mg/mL in EtOH with ultrasonic |
Chemical Name | (R)-4-((3-chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=CC(NC2=NC=NC3=CC(OC)=C(OC(N4[C@H](C)CN(C)CC4)=O)C=C23)=C1F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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