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AG490

Cat. No. M1646
AG490 Structure
Synonym:

Tyrphostin AG490

Size Price Availability Quantity
25mg USD 60 In stock
100mg USD 130 In stock
200mg USD 220 In stock
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Quality Control
Biological Activity

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.

Protocol
Cell Experiment
Cell lines ALL cells
Preparation method cell proliferation assay as described previously
Concentrations 0~50μM
Incubation time 16 h
Animal Experiment
Animal models ALL cells tumour xenograft SCID mice
Formulation DMSO
Dosages 0.85mg/kg +0.5mg/kg daily
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 294.30
Formula C17H14N2O3
CAS Number 133550-30-8
Purity 100%
Solubility DMSO ≥55 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source China Tropical Medicine (2017). Figure 5~6. AG490 (Abmole Bioscience, Shanghai, China)
Method
Cell Lines THP-1 cell
Concentrations 10 μmol/L
Incubation Time 30 min
Results The expression of NF-κB p65 protein in p-JAK2, p-STAT3 and nucleus was significantly lower than that in hypoxia group (P <0.05), while the expression of JAK2 and STAT3 The protein expression did not affect.
Rating
Source China Tropical Medicine (2017). Figure 1~4. AG490 (Abmole Bioscience, Shanghai, China)
Method
Cell Lines THP-1 cell
Concentrations 10 μmol/L
Incubation Time 30 min
Results The secretion and mRNA expression of IL-1β and TNF-α were significantly lower than those of hypoxia group (P <0.05), and the difference was statistically significant (P <0.05)
Rating
Source Int J Mol Med (2017) . Figure 6. AG490 (Abmole Bioscience, Houston, TX, USA)
Method qRT-PCR
Cell Lines Fibroblast-like synoviocytes (FLS)
Concentrations 25 μM
Incubation Time 24 h
Results Treatment with matrine, AG490, or matrine+AG490 markedly increased the mRNA expression of Bax and caspase-3, and decreased expression of Bcl-2 (P<0.01 vs. CIA alone).
Rating
Source Int J Mol Med (2017) . Figure 5. AG490 (Abmole Bioscience, Houston, TX, USA)
Method Western blot
Cell Lines Fibroblast-like synoviocytes (FLS)
Concentrations 25 μM
Incubation Time 24 h
Results Protein expression levels of p-JAK2, p-STAT1 and p-STAT3 in FLS isolated after 24 h of drug treatment were only faintly detectable in the control group, and markedly higher in the CIA group (P<0.01 vs. control; Fig. 5).
Rating
Source Int J Mol Med (2017) . Figure 4. AG490 (Abmole Bioscience, Houston, TX, USA)
Method propidium iodide (PI) staining and flow cytometry
Cell Lines Fibroblast-like synoviocytes (FLS)
Concentrations 25 μM
Incubation Time 24 h
Results All drug treatments resulted in signifcantly higher apoptosis rates than that observed for the CIA group (P<0.01; matrine, 20.10±0.77%; AG490, 20.42±0.91%; matrine+AG490, 25.11±1.00%).
Rating
Source Int J Mol Med (2017) . Figure 3. AG490 (Abmole Bioscience, Houston, TX, USA)
Method propidium iodide (PI) staining and flow cytometry
Cell Lines Fibroblast-like synoviocytes (FLS)
Concentrations 25 μM
Incubation Time 24 h
Results Compared with the CIA group, the percentages of FLS in the S phase were significantly decreased in cells treated with matrine, the specifc JAK2 inhibitor AG490 (inhibits phosphorylation of STAT1/3 in RA-FLS), or both for 24 h (P<0.01; Fig. 3).
Rating
Product Citations
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AG490, Tyrphostin AG490 supplier, JAK, inhibitors

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