658551

AG 1296

A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors and β-receptors.

• 同義詞: AG 1296, 6,7-Dimethoxy-3-phenylquinoxaline
• 經驗公式（希爾表示法）: C₁₆H₁₄N₂O₂
• CAS號碼: 146535-11-7
• 分子量：: 266.29
• MDL號碼: MFCD00270913
• 分類程式碼代碼: 12352200

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: white
• 溶解度: DMSO: 10 mg/mL; acetonitrile: soluble
• 運輸包裝: ambient
• 儲存溫度: −20°C
• InChI: 1S/C16H14N2O2/c1-19-15-8-12-13(9-16(15)20-2)18-14(10-17-12)11-6-4-3-5-7-11/h3-10H,1-2H3
• InChI 密鑰: QNOXYUNHIGOWNY-UHFFFAOYSA-N

描述

一般說明

Similar to but more potent than AG 1295 (Cat. No. 658550). A cell-permeable, reversible, and ATP-competitive, inhibitor of PDGF receptor kinase and blocks signaling of human PDGF α-receptors (IC₅₀ = 1.0 µM) and β-receptors (IC₅₀ = 800 nM) as well as of the related stem cell factor receptor c-kit (80% inhibition at 5 µM). Affects neither the binding of PDGF-BB to the PDGF-β receptor nor the receptor dimerization. Has no effect on autophosphorylation of the vascular endothelial growth factor receptor KDR or on DNA synthesis induced by vascular endothelial growth factor in porcine aortic endothelial cells. Also reverses the transformed phenotype of sis-transfected NIH/3T3 cells but has no effect on src-transformed NIH 3T3 cells or on the activity of the kinase p60^c-src (F257) immunoprecipitated from these cells. Potently inhibits autophosphorylation in Flt3/Tel-BaF3 and Flt3/Itd-BaF3 cells with an IC₅₀ of 300 nM and ~1 µM, respectively.

生化／生理作用

Cell permeable: yes

Primary Target
PDGFR kinase

Product competes with ATP.

Reversible: yes

Target IC₅₀: 1.0 µM, 800 nM, against signaling of human PDGF α-receptors, human PDGF β-receptors, respectively

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

其他說明

Tse, KF., et al. 2002. Leukemia16, 2027.
Tse, KF., et al. 2001. Leukemia15, 1001.
Strutz, F., et al. 2001. Kidney Int.59, 579.
Kovalenko, M., et al. 1997. Biochemistry 36, 6260.
Kovalenko, M., et al. 1994. Cancer Res. 54, 6106.

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