产品说明
一般描述
A cell-permeable bis(1H-2-indolyl)-1-methanone compound that acts as a highly selective, ATP-competitive and reversible inhibitor of platelet-derived growth factor (PDGF) receptor tyrosine kinase (IC50 = 1.1 M in Swiss 3T3 cells for PDGFR). Also potently inhibits Flt3 (Fms-like tyrosine kinase 3) activity (IC50 = 6.2 M for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells). Sensitizes 32D cells to radiation-induced apoptosis and inhibits proliferation of TEL-Flt3-transfected BA/F3 cells (IC50<300 nM). May also serve as a prodrug form of the Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I in cells.
Prodrug form of Platelet Derived Growth Factor Receptor Tyrosine Kinase Inhibitor I (Cat. No. 521230) that acts as a highly selective, cell-permeable, ATP-competitive, and reversible inhibitor of platelet-derived growth factor receptor (PDGFR) tyrosine kinase (IC50 = 1.1 µM, Swiss 3T3 cells). Also potently inhibits Fms-like tyrosine kinase 3 (Flt3) activity (IC50 = 6.2 µM for PDGFRβ-mFlt3 and 50 nM in EOL-1 cells). Reported to sensitize 32D cells to radiation-induced apoptosis. Also shown to inhibit proliferation of TEL-Flt3-transfected BA/F3 cells (IC50 >300 nM).
包装
1 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
PDGFR in swiss 3T3 cells
Product competes with ATP.
Reversible: yes
Target IC50: 1.1 µM inhibiting PDGFR in swiss 3T3 cells; 6.2 µ M for hPDGFβ-R-mFlt3 and 50 nM in EOL-1 cells
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Mahboobi, S., et al. 2002. J. Med. Chem.45, 1002.
Teller, S., et al. 2002. Leukemia16, 1528.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C21H18N2O3 |
分子量 | 346.38 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | yellow |
溶解性 | DMSO: 5 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 1 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |