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Saracatinib

Cat. No. 7189 1 条评论 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective Src tyrosine kinase family inhibitor; anticancer; antiviral; orally bioavailable
别名： AZD 0530
化学名： N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methyl-1-piperazinyl)ethoxy]-5-[(tetrahydro-2H-pyran-4-yl)oxy]-4-quinazolinamine
纯度： ≥98% (HPLC)
说明书
引用文献
评论 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for Saracatinib

Saracatinib is a potent and selective Src tyrosine kinase family inhibitor (IC50 = 4-10 nM). Inhibits Src, c-Yes, Fyn, Lyn, Blk, Fgr, and Lck. Exhibits selectivity over other tyrosine kinases (IC50 values are 30, 66 and 200 nM for v-Abl, EGFR and c-Kit, respectively). Suppresses invasion of HT1080 cells through a collagen matrix and inhibits metastasis in a murine model of bladder cancer. Inhibits the growth of prostate cancer cell lines. Also suppresses MERS-CoV replication at the early stage of replication (EC50 = 2.9 μM) and displays broad-spectrum activity against other human coronaviruses. Also blocks dengue virus RNA replication. Reverses memory deficit in a mouse AD model and rescues synapse density. Inhibits osteoclast activity, resorption and formation. Induces autophagy. Orally bioavailable.

化合物库 for Saracatinib

Saracatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。

技术数据 for Saracatinib

分子量 542.03
公式 C27H32ClN5O5
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 379231-04-6
PubChem ID 10302451
InChI Key OUKYUETWWIPKQR-UHFFFAOYSA-N
Smiles CN1CCN(CCOC2=CC3=C(C(NC4=C5OCOC5=CC=C4Cl)=NC=N3)C(OC3CCOCC3)=C2)CC1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Saracatinib

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 10.84 20
ethanol 54.2 100

制备储备液 for Saracatinib

以下数据基于产品分子量 542.03。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.84 mL 9.22 mL 18.45 mL
5 mM 0.37 mL 1.84 mL 3.69 mL
10 mM 0.18 mL 0.92 mL 1.84 mL
50 mM 0.04 mL 0.18 mL 0.37 mL

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产品说明书 for Saracatinib

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for Saracatinib

参考文献是支持产品生物活性的出版物。

Hennequin et al (2006) N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor. J.Med.Chem. 49 6465 PMID: 17064066

Green et al (2009) Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530. Mol.Oncol. 3 248 PMID: 19393585

De Wispelaere et al (2013) The small molecules AZD0530 and dasatinib inhibit dengue virus RNA replication via Fyn kinase. J.Virol. 87 7367 PMID: 23616652

Kaufman et al (2015) Fyn inhibition rescues established memory and synapse loss in Alzheimer mice. Ann.Neurol. 77 953 PMID: 25707991

If you know of a relevant reference for Saracatinib, please let us know.

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关键词: Saracatinib, Saracatinib supplier, AZD0530, AZD_0530, potent, selective, Src, tyrosine, kinase, family, inhibitors, inhibits, c-Yes, Fyn, Lyn, Blk, Fgr, Lck, MERS-cov, Covid-19, antiviral, dengue, viruses, AD, Alzheimers, disease, osteoclast, activity, AZD, 0530, Kinases, COVID-19, Coronavirus, 7189, Tocris Bioscience

篇 Saracatinib 的引用文献

引用文献是使用了 Tocris 产品的出版物。

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Saracatinib 的评论

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Saracatinib WB.
By Diego Vera on 08/19/2024
分析类型： In Vitro
种属： Human

A curve of Saracatinib was performed at different concentrations to standardize the working concentration for future assays at a specific incubation time established in our cell line. This was done by detecting the change in phosphorylated SRC levels compared to total SRC levels using western blot.

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