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.
Int Immunopharmacol. 2023 Feb;115:109693.
JAK2 inhibitor ameliorates the progression of experimental autoimmune myasthenia gravis and balances Th17/Treg cells via regulating the JAK2/STAT3-AKT/mTOR signaling pathway
AG490 purchased from AbMole
Int J Ophthalmol. 2022 Apr 18;15(4):554-559.
Leptin activates the JAK/STAT pathway to promote angiogenesis in RF/6A cells in vitro
AG490 purchased from AbMole
Int J Ophthalmol. 2022 Apr 18;15(4):554-559.
Leptin activates the JAK/STAT pathway to promote angiogenesis in RF/6A cells in vitro
AG490 purchased from AbMole
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
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
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
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. |
Molecular Weight | 294.30 |
Formula | C17H14N2O3 |
CAS Number | 133550-30-8 |
Solubility (25°C) | DMSO ≥45 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
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ZM39923
ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM. |
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