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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
AG-490 (also known as Tyrphostin B42; zinc-0255794) is a novel, potent and selective inhibitor of EGFR (epidermal growth factor receptor) with potential antitumor activities. It inhibits EGFR with an IC50 of 0.1 μM in cell-free assays, and shows 135-fold higher selectivity for EGFR over ErbB2. AG 490 also inhibits Janus kinase 2-JAK2 without inhibiting Lck, Lyn, Btk, Syk and Src.
| ln Vitro |
AG490 specifically blocks JAK2 to prevent Stat-3 from activating. JAK/Stat-3 activation is specifically inhibited by AG490. Cell viability is preserved and Stat-3 phosphorylation is reduced by more than 95% at a dosage of 10 μM. In EGF-stimulated A431 cells, 10 μM of AG490 causes a >95% drop in pStat-3 while having no effect on Stat-3 mass[1]. Strongly inhibiting the JAK3/STAT, JAK3/AP-1, and JAK3/MAPK pathways as well as their effects on cells is AG-490. In a dose-dependent manner, AG-490 eliminates IL-2-inducible [3H]thymidine incorporation with an IC50 of 25 μM. In contrast to earlier research that shown this drug triggered death in ALL cells while appearing to have no effect on the expansion of mitogen-stimulated normal T cells, AG-490 potently suppresses IL-2-mediated proliferation in T cells[2].
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| ln Vivo |
Type 1 diabetes (T1D) is substantially prevented by AG490 (p = 0.02, p = 0.005; at two distinct time points). In contrast to the absolute inability (0%; 0/10, p=0.003, Log-rank test) of DMSO, monotherapy with AG490 (1 mg/mouse) for newly diagnosed diabetic NOD mice significantly results in disease remission in treated animals (n=23), and sustained eugluycemia is maintained for several months after drug withdrawal[3]. In a dose-dependent manner, AG490 (1–10 µg) greatly reduces the thermal hyperalgesia caused by ʎ-carrageenan. Moreover, AG490 lessens mechanical hyperalgesia[4].
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Tyrphostin B42 has known human metabolites that include Tyrphostin B42, 4-O-glucuronide and Tyrphostin B42, 3-O-glucuronide. |
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| References |
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| Additional Infomation |
Tyrphostin B42 is a monocarboxylic acid amide obtained by formal condensation of the carboxy group of (2E)-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enoic acid with the amino group of benzylamine. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an antioxidant, a STAT3 inhibitor, an anti-inflammatory agent, an apoptosis inducer and a geroprotector. It is an enamide, a monocarboxylic acid amide, a nitrile, a member of catechols and a secondary carboxamide.
Tyrphostin B42 is a member of the tyrphostin family of tyrosine kinase inhibitors that inhibits epidermal growth factor receptor, blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of Mycosis fungoides tumor cells. (NCI) |
| Molecular Formula |
C17H14N2O3
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|---|---|
| Molecular Weight |
294.30
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| Exact Mass |
294.1
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| CAS # |
133550-30-8
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| Related CAS # |
(E/Z)-AG490;134036-52-5
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| PubChem CID |
5328779
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
615.2±55.0 °C at 760 mmHg
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| Melting Point |
215°C(lit.)
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| Flash Point |
325.9±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.679
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| LogP |
2.11
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
460
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)CNC(=O)/C(=C/C2=CC(=C(C=C2)O)O)/C#N
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| InChi Key |
TUCIOBMMDDOEMM-RIYZIHGNSA-N
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| InChi Code |
InChI=1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+
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| Chemical Name |
(E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide
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| Synonyms |
Zinc-0255794; Tyrphostin AG490; Zinc0255794; Zinc 0255794; Tyrphostin AG-490; AG 490; AG-490; AG490; Tyrphostin AG 490
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.07 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (7.07 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Stat3 is activated in murine myeloma/plasmacytoma cell lines, and AG-490 treatment inhibits Stat3 DNA-binding activity.Mol Cancer Ther.2002 Sep;1(11):893-9. |
Administration of AG-490 inhibits activated Stat3, causes transient regression of murine myeloma/plasmacytoma tumors, and induces apoptosis of tumor cells in vivo.Mol Cancer Ther.2002 Sep;1(11):893-9. |
rIL-12 prolongs the AG-490-mediated antitumor effect.Mol Cancer Ther.2002 Sep;1(11):893-9. |
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