Saracatinib (AZD0530)
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.
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. 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
- 3. 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
- 4. 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
- 5. 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
- 6. 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
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