Saracatinib (AZD0530) (Synonyms: AZD 0530) |
| رقم الكتالوجGC15197 |
Saracatinib (AZD0530) (AZD0530) هو مثبط قوي لعائلة Src مع IC50s من 2.7 إلى 11 نانومتر لـ c-Src و Lck و c-YES و Lyn و Fyn و Fgr و Blk. يُظهر Saracatinib (AZD0530) انتقائية عالية على كينازات التيروزين الأخرى.
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Cas No.: 379231-04-6
Sample solution is provided at 25 µL, 10mM.
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Saracatinib (AZD0530) is a novel, potent Src family kinase (SFK)/Abl dual-kinase inhibitor with IC50 value of 2.7 nM [1].
Saracatinib has been reported to inhibit Src activation in DU145 and PC3 cell lines (prostate cancer cell lines). Both of c-Myc and cyclin D1 expression are decreased by Saracatinib. Saracatinib can inhibit the ERK1/2 and GSK3b phosphorylation as well as decrease β-catenin level in cells. Saracatinib inhibits the prostate tumor cell growth by inducing cycle arrest at G1/S phase. Saracatinib dose-dependently blocks cell migration in DU145 and PC3 cell lines [1].
In DU145 implanted orthotopic SCID mice model, treatment with Saracatinib has been demonstrated to down-regulate the Src expression as well as suppress the tumor size [1].
References:
[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.
| Cell experiment: [1] | |
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Cell lines |
A549 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μM, 24 hours for cell migration inhibition 48 hours for cell invasion inhibition |
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Applications |
A549 cells were grown to confluent monolayers, which were scratched with a pipette tip and incubated with AZD0530 at concentrations ranging from 100 to 1000 nM. DMSO treated control cells continuously migrated into the scratch and nearly closed the scratch within 24 hours. Cell migration was significantly inhibited by AZD0530 in a dose-dependent way. At the highest dose tested (1 μM), AZD0530 reduced A549 cell migration by more than 60%. Cell invasion was tested using a modified Matrigel assay with A549 cells. AZD0530 significantly reduced Matrigel invasion in A549 cells by 51%. |
| Animal experiment: [2] | |
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Animal models |
Female athymic nude mice injected with Panc410 cells |
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Dosage form |
Oral administration, 50mg/kg/d for 28 days |
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Applications |
AZD0530 administration clearly down-regulated Src, FAK, p-FAK, and pSTAT-3 expression in the sensitive tumor (Panc410) compared with control tumors. In addition, AZD0530 administration resulted in the down-regulation of XIAP as evidenced by the immunoblot of Panc410. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 379231-04-6 | SDF | |
| المرادفات | AZD 0530 | ||
| Chemical Name | N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-(oxan-4-yloxy)quinazolin-4-amine | ||
| Canonical SMILES | CN1CCN(CC1)CCOC2=CC(=C3C(=C2)N=CN=C3NC4=C(C=CC5=C4OCO5)Cl)OC6CCOCC6 | ||
| Formula | C27H32ClN5O5 | M.Wt | 542.03 |
| الذوبان | ≥ 27.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8449 mL | 9.2246 mL | 18.4492 mL |
| 5 mM | 0.369 mL | 1.8449 mL | 3.6898 mL |
| 10 mM | 0.1845 mL | 0.9225 mL | 1.8449 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 6 reference(s) in Google Scholar.)
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