Saracatinib (AZD0530)
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Saracatinib(AZD0530)是一种新型有效的Src家族激酶(SFK)/Abl双重抑制剂,IC50值为2.7 nM[1]。
据报道,在DU145和PC3前列腺癌细胞系中,Saracatinib抑制Src的激活,通过诱导G1/S期细胞周期停滞抑制细胞生长,阻止细胞迁移。Saracatinib还可以减少c-Myc和cyclin D1的表达,抑制ERK1/2和GSK3b的磷酸化,减少β连环蛋白(β-catenin)的水平[1]。
在DU145原位移植SCID小鼠模型中,Saracatinib下调Src的表达,抑制肿瘤生长[1]。
参考文献:
[1] Chang YM1,?Bai L,?Liu S,?Yang JC,?Kung HJ,?Evans CP. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene.?2008 Oct 23;27(49):6365-75.
- 1. Xu Wang, Xinfang Yu, et al. "Expanding anti-CD38 immunotherapy for lymphoid malignancies." J Exp Clin Cancer Res. 2022 Jun 28;41(1):210 PMID: 35765110
- 2. Christopher M Dustin, Aida Habibovic, et al. "Oxidation–Dependent Activation of Src Kinase Mediates Epithelial IL-33 Production and Signaling during Acute Airway Allergen Challenge." J Immunol. 2021 Jun 15;206(12):2989-2999. PMID: 34088769
- 3. Liao X, Song G, et al. "Oxaliplatin resistance is enhanced by saracatinib via upregulation Wnt-ABCG1 signaling in hepatocellular carcinoma." BMC Cancer. 2020;20(1):31. PMID: 31931755
- 4. Panagi I, Jennings E, et al. "Salmonella Effector SteE Converts the Mammalian Serine/Threonine Kinase GSK3 into a Tyrosine Kinase to Direct Macrophage Polarization." Cell Host Microbe. 2020;27(1):41–53.e6. PMID: 31862381
- 5. Alzubi MA, Turner TH, et al. "Separation of breast cancer and organ microenvironment transcriptomes in metastases." Breast Cancer Res. 2019 Mar 6;21(1):36. PMID: 30841919
- 6. Nakachi I, Helfrich BA, et al. "PTTG1 Levels Are Predictive of Saracatinib Sensitivity in Ovarian Cancer Cell Lines." Clin Transl Sci. 2016 Dec;9(6):293-301. PMID: 27766744
- 7. Diao Y, Ma X, et al. "Dasatinib promotes paclitaxel-induced necroptosis in lung adenocarcinoma with phosphorylated caspase-8 by c-Src." Cancer Lett. 2016 May 16. PMID: 27195913
Storage | Store at -20°C |
M.Wt | 542.03 |
Cas No. | 379231-04-6 |
Formula | C27H32ClN5O5 |
Solubility | ≥27.1 mg/mL in DMSO; insoluble in EtOH; ≥2.36 mg/mL in H2O with ultrasonic |
Chemical Name | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine |
SDF | Download SDF |
Canonical SMILES | CN1CCN(CC1)CCOC2=CC(=C3C(=C2)N=CN=C3NC4=C(C=CC5=C4OCO5)Cl)OC6CCOCC6 |
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。 |
细胞实验[1]: | |
细胞系 |
A549细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
1 μM,细胞迁移抑制:24 h;细胞侵袭抑制:48 h。 |
应用 |
A549细胞生长形成融合单层,移液器尖端划伤后用100-1000 nM的AZD0530孵育。在24小时内,DMSO处理的对照细胞持续迁移进入划伤区域,几乎完全覆盖了划痕。AZD0530以剂量依赖的方式显著抑制细胞迁移。在检测的最高浓度(1 μM),AZD0530减少了超过60%的A549细胞迁移。用修改的基底膜实验检测A549细胞的侵袭,AZD0530显著减少了51%的基底膜侵袭。 |
动物实验[2]: | |
动物模型 |
植入Panc410细胞的雌性无胸腺裸鼠 |
剂量 |
50mg/kg/d,28天;口服给药 |
应用 |
与对照肿瘤相比,在敏感肿瘤Panc410中,AZD0530明显减少Src、FAK、p-FAK和pSTAT-3的表达。此外,AZD0530导致XIAP的下调,正如Panc410的免疫印迹结果所示。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Purnell P R, Mack P C, Tepper C G, et al. The Src inhibitor AZD0530 blocks invasion and may act as a radiosensitizer in lung cancer cells. Journal of thoracic oncology: official publication of the International Association for the Study of Lung Cancer, 2009, 4(4): 448. [2] Rajeshkumar N V, Tan A C, De Oliveira E, et al. Antitumor effects and biomarkers of activity of AZD0530, a Src inhibitor, in pancreatic cancer. Clinical Cancer Research, 2009, 15(12): 4138-4146. |
描述 | Saracatinib (AZD0530)是一种有效的Src抑制剂,IC50值为2.7 nM,对c-Yes、 Fyn、Lyn、Blk、Fgr和Lck也具有活性,对Abl和EGFR (L858R和L861Q)活性较低。 | |||||
靶点 | c-Src | v-Abl | ||||
IC50 | 2.7 nM | 30 nM |
质量控制和MSDS
- 批次:
化学结构
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