AG-490 (Tyrphostin B42) (Synonyms: Tyrphostin AG-490) |
| カタログ番号GC13854 |
AG-490 (Tyrphostin B42)はEGFRの阻害剤であり、IC50の値は0.1µMであり、AG-490はJAK2に対する阻害作用もある。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 133550-30-8
Sample solution is provided at 25 µL, 10mM.
AG-490 (Tyrphostin B42)はEGFRの阻害剤であり、IC50の値は0.1µMであり、AG-490はJAK2に対する阻害作用もある[1-3]。
AG-490（5-50µM；3日間）はRAW264.7細胞におけるRANKL誘発した破骨細胞産生を阻害できる[4]。AG490(20µM;4h)はhOAT3の輸送の活性を阻害する[5]。AG-490(10µM)は鼠の骨髄マクロファージにおけるインターロイキン34が媒介した破骨細胞の形成を阻害できる[6]。
AG-490(5-15 µM;i.p;)は体内神経細胞のアポトーシスを阻止することで保護作用を果たす[7]。腫瘍鼠では、AG-490（500µg/マウス；腹腔注射；11日間）治療は皮下腫瘍の成長を顕著に阻害できる[8]。
References:
[1]. DuhÉ RJ, Clark EA, et,al. Characterization of the in vitro kinase activity of a partially purified soluble GST/JAK2 fusion protein. Mol Cell Biochem. 2002 Jul;236(1-2):23-35. doi: 10.1023/a:1016186907376. PMID: 12190118.
[2]. Luo C, Laaja P. Inhibitors of JAKs/STATs and the kinases: a possible new cluster of drugs. Drug Discov Today. 2004 Mar 15;9(6):268-75. doi: 10.1016/S1359-6446(03)03014-9. PMID: 15003245.
[3]. Gazit A, Osherov N, et,al. Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases. J Med Chem. 1991 Jun;34(6):1896-907. doi: 10.1021/jm00110a022. PMID: 1676428.
[4]. Li CH, Zhao JX, et,al. AG490 inhibits NFATc1 expression and STAT3 activation during RANKL induced osteoclastogenesis. Biochem Biophys Res Commun. 2013 Jun 14;435(4):533-9. doi: 10.1016/j.bbrc.2013.04.084. Epub 2013 May 7. PMID: 23665018.
[5]. Zhang J, Liu C, et,al. AG490, a JAK2-specific inhibitor, downregulates the expression and activity of organic anion transporter-3. J Pharmacol Sci. 2018 Mar;136(3):142-148. doi: 10.1016/j.jphs.2018.01.006. Epub 2018 Feb 8. PMID: 29487013; PMCID: PMC7863619.
[6]. Cheng X, Wan QL, et,al. AG490 suppresses interleukin-34-mediated osteoclastogenesis in mice bone marrow macrophages. Cell Biol Int. 2017 Jun;41(6):659-668. doi: 10.1002/cbin.10771. Epub 2017 Apr 19. PMID: 28378938.
[7]. Fan L, Zhou L. AG490 protects cerebral ischemia/reperfusion injury via inhibiting the JAK2/3 signaling pathway. Brain Behav. 2021 Jan;11(1):e01911. doi: 10.1002/brb3.1911. Epub 2020 Oct 23. PMID: 33098244; PMCID: PMC7821583.
[8]. Kobayashi A, Tanizaki Y, et,al. AG490, a Jak2 inhibitor, suppressed the progression of murine ovarian cancer. Eur J Pharmacol. 2015 Nov 5;766:63-75. doi: 10.1016/j.ejphar.2015.09.039. Epub 2015 Sep 26. PMID: 26410360.
| 細胞実験[1]: | |
細胞株 | RAW264.7細胞 |
準備方法 | RANKL (100 ng/mL) および漸増濃度の AG-490 の存在下で細胞を培養する。 |
反応条件 | 5-50μM;3日 |
アプリケーション | AG-490はRAW264.7細胞におけるRANKL誘発した破骨細胞産生を阻害できる |
| 動物実験 [2]: | |
動物モデル | メスB6C3F1鼠(HM-1癌モデル) |
準備方法 | 鼠に毎日AG-490（500 μ g/鼠）を腹腔内注射する、または对照として単独PBSでする。 |
投与形態 | 500μg/鼠; i.p;11日間 |
アプリケーション | 対照群に比べると、AG-490治療は皮下腫瘍の成長を顕著に阻害する。 |
| References: [1]. Li CH, Zhao JX, et,al. AG490 inhibits NFATc1 expression and STAT3 activation during RANKL induced osteoclastogenesis. Biochem Biophys Res Commun. 2013 Jun 14;435(4):533-9. doi: 10.1016/j.bbrc.2013.04.084. Epub 2013 May 7. PMID: 23665018. | |
| Cas No. | 133550-30-8 | SDF | |
| 同義語 | Tyrphostin AG-490 | ||
| Chemical Name | (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide | ||
| Canonical SMILES | C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N | ||
| Formula | C17H14N2O3 | M.Wt | 294.3 |
| 溶解度 | Soluble in DMSO > 10 mM | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.3979 mL | 16.9895 mL | 33.9789 mL |
| 5 mM | 0.6796 mL | 3.3979 mL | 6.7958 mL |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3979 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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
-
Related Biological Data
Effect of LBPE on JAK2/STAT3 Signal Pathway in H9c2 Cells. (C) Gene expression of ANP when treated with LBPE (500 μg∙mL−1) and/or AG490 (10 μmol∙L−1).
Cells were incubated with AG490(GLPBIO) for 30 min before ISO injury to verify the effects of JAK2-blockage on ISO-induced CH.
Antioxidants 12.1 (2023): 88. PMID: 36670950 IF: 7.6745 -
Related Biological Data
Naringin promotes BMSC viability and osteogenic differentiation. (B) Alizarin red staining was employed for detecting the formation of calcium mineral deposits after naringin (100 μg/ml) or AG490 treatment, which revealed osteogenic differentiation of BMSCs.
Rats in the PMOP+AG490(GlpBio) group were ovariectomized and administered intraperitoneally with 10 μg of AG490 (40) 3 times each week.
Clin Exp Pharmacol P (2021). PMID: 34525226 IF: 2.553
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *