658401

AG 490

A cell-permeable, reversible, substrate competitive, and potent inhibitor of epidermal growth factor receptor kinase autophosphorylation (IC₅₀ = 100 nM).

• 同義詞: AG 490, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, ( E)- N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI, α-Cyano-(3,4-dihydroxy)-N-benzylcinnamide, Tyrphostin B42, (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)acrylamide, JAK1 Inhibitor II, JAK2 Inhibitor VI, JAK3 Inhibitor XI
• 經驗公式（希爾表示法）: C₁₇H₁₄N₂O₃
• CAS號碼: 133550-30-8
• 分子量：: 294.30
• MDL號碼: MFCD00236452
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: yellow
• 溶解度: DMSO: 100 mg/mL
• 運輸包裝: ambient
• 儲存溫度: −20°C
• SMILES 字串: 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 密鑰: TUCIOBMMDDOEMM-RIYZIHGNSA-N

描述

一般說明

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.

生化／生理作用

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

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

其他說明

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.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3