AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase with an IC50 values of 2 and 13.5 μM for EGFR and ErbB2 respectively. AG490 is also a JAK3/STAT, JAK3/AP-1 and JAK3/MAPK signaling pathway inhibitor and also blocks JAK3 autophosphorylation. AG-490 significantly inhibits the constitutive activation of Stat3 in MOPC, MPC11, and S194 cells, leading to dramatic dose-dependent apoptosis. AG-490 (100 μM) inhibits Akt phosphorylation, inhibits the activation of nuclear factor-κB, and causes the activation of GSK-3β, leading to the reduction of c-Myc. AG-490 (50 μM) can induce apoptosis of imatinib-resistant BaF3 cells expressing T315I and E255K mutants of Bcr-Abl.
J Tradit Chin Med. 2019 April 15;39(2): 181-190.
Efficacy of Zhonglun'a-decoction-containing serum on fibroblast-like synoviocyte apoptosis in rats with collagen-induced arthritis via inhibiting Janus kinase/signal transducer and activator of transcription signaling pathway.
AG490 purchased from AbMole
Med Sci Monit. 2018 Sep 8;24:6255-6263.
Inhibition of JAK2/STAT3 Signaling Pathway Suppresses Proliferation of Burkitt's Lymphoma Raji Cells via Cell Cycle Progression, Apoptosis, and Oxidative Stress by Modulating HSP70.
AG490 purchased from AbMole
Nutr Res. 2018 Mar 18.
Folic acid supplementation repressed hypoxia-induced inflammatory response via ROS and JAK2/STAT3 pathway in human pro-myelomonocytic cells
AG490 purchased from AbMole
Int J Mol Med. 2017 Feb;39(2):307-316.
Matrine induces the apoptosis of fibroblast-like synoviocytes derived from rats with collagen-induced arthritis by suppressing the activation of the JAK/STAT signaling pathway
AG490 purchased from AbMole
Cell Experiment | |
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Cell lines | ALL cells |
Preparation method | cell proliferation assay as described previously |
Concentrations | 0~50μM |
Incubation time | 16 h |
Animal Experiment | |
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Animal models | ALL cells tumour xenograft SCID mice |
Formulation | DMSO |
Dosages | 0.85mg/kg +0.5mg/kg daily |
Administration | i.p. |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Molecular Weight | 294.30 |
Formula | C17H14N2O3 |
CAS Number | 133550-30-8 |
Purity | 100.0% |
Solubility | DMSO ≥45 mg/mL |
Storage | at -20°C |
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