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EGFR Inhibitor II, BIBX1382-CAS 196612-93-8-Calbiochem
| 产品编号： | 4083833 |
| 规格： | The EGFR Inhibitor II, BIBX1382, also referenced under CAS 196612-93-8, controls the biological activity of EGFR. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| CAS NO： | 196612-93-8 |
| 包装规格： | 5 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
196612-93-8
EGFR Inhibitor II, BIBX1382-CAS 196612-93-8-Calbiochem
N8-(3-Chloro-4-fluorophenyl)-N2-(1-methylpiperidin-4-yl)-pyrimido[5,4-d]pyrimidine-2,8-diamine, 2HCl, BIBX1382BS
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H19ClFN7 · 2HCl · 2H2O |
| Molecular weight | 496.79 |
| General description【一般描述】 | A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (10 mg/kg, daily, p.o.). A cell-permeable pyrimidopyrimidine compound that acts as a potent, reversible, ATP-competitive, and highly selective inhibitor of EGFR (ErbB-1, HER-1) both in cell-free enzymatic reactions (IC50 = 3 nM) and in culture (IC50 = 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells). It exhibits 1,000-fold greater selectivity over ErbB-2 (HER-2, neu; IC50 = 3.4 µM) and shows little activity towards IGF1R, β-InsRK, HGFR, c-src, and VEGFR-2 even at concentrations as high as 10 µM. Its antitumor efficacy has also been demonstrated in a murine xenograft model in vivo (daily p.o. dose 10 mg/kg). |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Target IC50: 3 nM against EGFR (ErbB-1, HER-1) in cell-free enzymatic reactions; 0.15, 1.82, and 3.2 µM in EGF-, HGF-, and FCS-dependent thymidine incorporation, respectively, in KB cells Primary Target EGFR (ErbB-1, HER-1) Product competes with ATP. Reversible: yes |
| Warning【警告】 | Toxicity: Irritant (B) |
| Other Notes【其他说明】 | Solca, F.F., et al. 2004. J. Pharm. Exp. Ther.311, 502. Egeblad, M., et al. 2001. Biochem. Biophys. Res. Commun.281, 25. Nuijen, B., et al. 2000. Int. J. Pharm.194, 261. Tocris suggests 50 mM solution can be made in water or DMSO. Aliquot & store at -20*C; stable for 6 months. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
| color【颜色】 | yellow |
| solubility【溶解性】 | water: 1 mg/mL DMSO: 25 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | 5 mg in Plastic ampoule |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 2 |
