Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A126525-20mg | 20mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $46.90 | |
A126525-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $96.90 | |
A126525-250mg | 250mg | In stock | $436.90 | |
A126525-1g | 1g | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $1,571.90 |
JAK2/3 inhibitor
Synonyms | BS-15205 | C72336 | EX-A118 | NCGC00016014-03 | SR-01000076153-3 | (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide | IDI1_033866 | SMP2_000154 | Diflunisalum [INN-Latin] | s1143 | HMS1361F18 | BMK1-D1 | NCGC00016014-07 | SR-01000076153 | EU-010 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | AG-490 is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). Inhibitor of JAK2, JAK3/STAT, JAK3/AP-1 and JAK3/MAPK pathways and potently inhibits cytokine-independent cell growth in vi |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of epidermal growth factor receptor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Toxic, refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
Product Description | AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR with IC50 of 0.1 μM, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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Pubchem Sid | 488195367 |
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Pubchem Sid Url | https://pubchem.ncbi.nlm.nih.gov/substance/488195367 |
IUPAC Name | (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide |
INCHI | 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+ |
InChi Key | TUCIOBMMDDOEMM-RIYZIHGNSA-N |
Canonical SMILES | C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N |
Isomeric SMILES | C1=CC=C(C=C1)CNC(=O)/C(=C/C2=CC(=C(C=C2)O)O)/C#N |
WGK Germany | 3 |
PubChem CID | 5328779 |
Molecular Weight | 294.3 |
PubChem CID | 5328779 |
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CAS Registry No. | 133550-30-8 |
ChEMBL Ligand | CHEMBL56543 |
PubChem SID | 488195367 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
C23031333 | Certificate of Analysis | Dec 06, 2024 | A126525 |
C2313133 | Certificate of Analysis | Mar 22, 2023 | A126525 |
J1711005 | Certificate of Analysis | Mar 17, 2023 | A126525 |
C2131104 | Certificate of Analysis | Jan 13, 2023 | A126525 |
Solubility | DMSO ≥57mg/mL Water <1.2mg/mL Ethanol ≥8mg/mL |
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Sensitivity | Light Sensitive,Air Sensitive,Heat Sensitive |
Melt Point(°C) | 215°C |
Pictogram(s) | GHS06, GHS09 |
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Signal | Danger |
Hazard Statements | H301:Toxic if swallowed H400:Very toxic to aquatic life |
Precautionary Statements | P273:Avoid release to the environment. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P301+P316:IF SWALLOWED: Get emergency medical help immediately. |
WGK Germany | 3 |
1. Suwen Liu, Wenhong Jiang, Chang Liu, Shuo Guo, Hao Wang, Xuedong Chang. (2023) Chinese chestnut shell polyphenol extract regulates the JAK2/STAT3 pathway to alleviate high-fat diet-induced, leptin-resistant obesity in mice. Food & Function, 14 (10): (4807-4823). [PMID:37128963] [10.1039/D3FO00604B] |
2. Suwen Liu, Zhang Lu, Chang Liu, Xuedong Chang, Buhailiqiemu Apudureheman, Shiguo Chen, Xingqian Ye. (2022) Castanea mollissima shell polyphenols regulate JAK2 and PPARγ expression to suppress inflammation and lipid accumulation by inhibiting M1 macrophages polarization. Journal of Functional Foods, 92 (105046). [PMID:] [10.1016/j.jff.2022.105046] |
1. Gazit A, Osherov N, Posner I, Yaish P, Poradosu E, Gilon C, Levitzki A. (1991) Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.. J Med Chem, 34 (6): (1896-907). [PMID:1676428] [10.1021/op500134e] |
2. Zeng Y et al.. (2014) Inhibition of STAT5a by Naa10p contributes to decreased breast cancer metastasis.. Carcinogenesis, 35 (10): (2244-53). [PMID:24925029] |
3. Wang Y & Li Y. (2018) MiR-29c inhibits HCV replication via activation of type I IFN response by targeting STAT3 in JFH-1-infected Huh7 cells.. RSC Adv, 8 (15): (8164-8172). [PMID:35542013] |
4. Zhang Z et al.. (2021) Neuritin inhibits astrogliosis to ameliorate diabetic cognitive dysfunction.. J Mol Endocrinol, 66 (4): (259-272). [PMID:33729996] |
5. Li HN et al.. (2021) Red nucleus IL-33 facilitates the early development of mononeuropathic pain in male rats by inducing TNF-a through activating ERK, p38 MAPK, and JAK2/STAT3.. J Neuroinflammation, 18 (150). [PMID:34225736] |
6. Guo YJ et al.. (2018) Red nucleus interleukin-1ß evokes tactile allodynia through activation of JAK/STAT3 and JNK signaling pathways.. J Neurosci Res, 96 (12): (1847-1861). [PMID:30216497] |
7. Suwen Liu, Wenhong Jiang, Chang Liu, Shuo Guo, Hao Wang, Xuedong Chang. (2023) Chinese chestnut shell polyphenol extract regulates the JAK2/STAT3 pathway to alleviate high-fat diet-induced, leptin-resistant obesity in mice. Food & Function, 14 (10): (4807-4823). [PMID:37128963] [10.1039/D3FO00604B] |
8. Suwen Liu, Zhang Lu, Chang Liu, Xuedong Chang, Buhailiqiemu Apudureheman, Shiguo Chen, Xingqian Ye. (2022) Castanea mollissima shell polyphenols regulate JAK2 and PPARγ expression to suppress inflammation and lipid accumulation by inhibiting M1 macrophages polarization. Journal of Functional Foods, 92 (105046). [PMID:] [10.1016/j.jff.2022.105046] |