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.
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Molecular Weight | 294.30 |
Formula | C17H14N2O3 |
CAS Number | 133550-30-8 |
Purity | 100% |
Solubility | DMSO ≥55 mg/mL |
Storage | at -20°C |
AG490 Promotes HIF-1α Accumulation by Inhibiting Its Hydroxylation.
Fernandez-Sanchez et al. Curr Med Chem. 2012 Aug 1;19(23):4014-23. PMID: 22709000.
Tyrphostin AG490 Agent Modestly but Significantly Prevents Onset of Type 1 in NOD Mouse; Implication of Immunologic and Metabolic Effects of a Jak-Stat Pathway Inhibitor.
Davoodi-Semiromi et al. J Clin Immunol. 2012 Jun 4. PMID: 22661285.
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FLLL32
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