- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC50 = 100 nM). Inhibition of JAK2 by AG 490 selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. Inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. AG 490 has also been shown to inhibit the autokinase activity of JAK3. A 100 mM (5 mg/170 µl) solution of AG490 (Cat. No. 658411) in DMSO is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
epidermal growth factor receptor kinase autophosphorylation
Product does not compete with ATP.
Reversible: yes
Target IC50: 100 nM against epidermal growth factor receptor kinase autophosphorylation
Preparation Note
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
Other Notes
Jaleel, M., et al. 2004. Biochemistry43, 8247.
Eriksen, K.W., et al. 2001. Leukemia15, 787.
Kirken, R.A., et al. 1999. Leukoc. Biol.65, 891.
Nielsen, M., et al. 1997. Proc. Natl. Acad. Sci. USA 94, 6764.
Meydan, N., et al. 1996. Nature 379, 645.
Gazit, A., et al. 1991. J. Med. Chem.34, 1896.
Levitzki, A. 1990. Biochem. Pharmacol.40, 913.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | yellow |
| solubility | DMSO: 100 mg/mL |
| web metadata keyword.default | 100 nM AG 490 potency,AG 490 IL-2 induced growth blocker,AG 490 JAK2 inhibitor 100 nM,AG 490 JAK3 inhibitor XI,AG 490 STAT-3 DNA binding inhibitor,AG 490 alpha-cyano-(3,4-dihydroxy)-N-benzylcinnamide,AG 490 cell-permeable inhibitor,AG 490 epidermal growth factor receptor kinase inhibitor,AG 490 for leukemic cell growth inhibition,AG 490 for programmed cell death research,AG 490 laboratory-grade inhibitor,AG 490 titration reagent,AG 490,reversible JAK2 inhibitor AG 490 |
| shipped in | ambient |
| storage temp. | −20°C |
| SMILES string | N(Cc2ccccc2)C(=O)\C(=C\c1cc(c(cc1)O)O)\C#N |
| 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 |
| 长度(mm) | |
| 宽度(mm) | |
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| 重量(kg) |




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