AG 825 (Synonyms: Tyrphostin AG825) |
| カタログ番号GC13168 |
AG 825 (Tyrphostin AG 825) は、0.35 μM の IC50 でチロシンリン酸化を抑制する、選択的かつ ATP 競合的な ErbB2 阻害剤です。
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Cas No.: 149092-50-2
Sample solution is provided at 25 µL, 10mM.
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AG 825 is a selective inhibitor of ErbB2 with IC50 values of 0.15 and 19 μM for ErbB2 and ErbB1 respectively [1].
Receptor tyrosine-protein kinase erbB-2 is a member of the human epidermal growth factor receptor family and promotes cell proliferation.
AG 825 is a selective ErbB2 inhibitor. AG825 inhibited autophosphorylation of HER2, HER1-2 and HER1 with IC50 values of 0.15, 0.35 and 19 μM, respectively [1]. In non-small cell lung cancer (NSCLC) cell lines expressing high-p185neu, the HER-2/neu gene product, AG825 significantly increased the chemosensitivities. However, AG825 with high concentrations inhibited the drug-induced G2 arrest and the activation of phosphorylated p34cdc2 [2]. In androgen-independent prostate cancer (PCa) cell lines C4 and C4-2, AG825 was toxic in a dose- and time-dependent way and inhibited phosphoactivation of HER-2/neu and its down-regulation. Also, AG825 induced an imbalance between p38 mitogen-activated protein kinase activation and extracellular signal-regulated kinase 1/2, which then led to p38-dependent apoptosis [3].
References:
[1]. Osherov N, Gazit A, Gilon C, et al. Selective inhibition of the epidermal growth factor and HER2/neu receptors by tyrphostins. J Biol Chem, 1993, 268(15): 11134-11142.
[2]. Tsai CM, Levitzki A, Wu LH, et al. Enhancement of chemosensitivity by tyrphostin AG825 in high-p185(neu) expressing non-small cell lung cancer cells. Cancer Res, 1996, 56(5): 1068-1074.
[3]. Murillo H, Schmidt LJ, Tindall DJ. Tyrphostin AG825 triggers p38 mitogen-activated protein kinase-dependent apoptosis in androgen-independent prostate cancer cells C4 and C4-2. Cancer Res, 2001, 61(20): 7408-7412.
| Cas No. | 149092-50-2 | SDF | |
| 同義語 | Tyrphostin AG825 | ||
| Chemical Name | (E)-3-(3-((benzo[d]thiazol-2-ylthio)methyl)-4-hydroxy-5-methoxyphenyl)-2-cyanoacrylamide | ||
| Canonical SMILES | OC(C(CSC1=NC2=CC=CC=C2S1)=CC(/C=C(C#N)/C(N)=O)=C3)=C3OC | ||
| Formula | C19H15N3O3S2 | M.Wt | 397.47 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO: PBS (pH 7.2)(1:3): 0.1 mg/ml,Ethanol: 0.2 mg/ml | 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 | 2.5159 mL | 12.5796 mL | 25.1591 mL |
| 5 mM | 0.5032 mL | 2.5159 mL | 5.0318 mL |
| 10 mM | 0.2516 mL | 1.258 mL | 2.5159 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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