| 溶解性 | DMSO 88 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 产品介绍 | AEE788(NVP-AEE 788)是高活性的EGFR和HER2/ErbB2抑制剂，IC50分别为2 nM和6 nM，对VEGFR2/KDR，c-Abl，c-Src和Flt-1抑制性较弱，对Ins-R，IGF-1R, PKCα and CDK1无抑制性。 |
| 备注 | AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. |
| 生化机理 | Description:IC50 Value: 2 nM( EGFR); 6 nM (ErbB2) [1]AEE788 is a novel dual specific receptor tyrosine kinase inhibitor. AEE788, obtained by optimization of the 7H-pyrrolo[2,3-d]pyrimidine lead scaffold, is a potent combined inhibitor of both epidermal growth factor (EGF) and VEGF receptor tyrosine kinase family members.in vitro: At the enzyme level, AEE788 inhibited EGFR and VEGF receptor tyrosine kinases in the nm range (IC(50)s: EGFR 2 nm, ErbB2 6 nm, KDR 77 nm, and Flt-1 59 nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited (IC(50)s: 11 and 220 nm, respectively)[1]. Treatment of cutaneous SCC cells with AEE788 led to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis [2].in vivo: Oral administration of AEE788 to tumor-bearing mice resulted in high and persistent compound levels in tumor tissue. Moreover, AEE788 efficiently inhibited grow |
| 别名 | AEE-788;AEE 788;NVP-AEE 788;6-[4-[(4-乙基-1-哌嗪)甲基]苯基]-N-[(1R)-1-苯基乙基]-7H-吡咯并[2,3-d]嘧啶-4-胺;AEE-788;AEE 788;NVP-AEE 788; 6-{4-[(4-Ethyl-1-piperazinyl)methyl]phenyl}-N-[(1R)-1-phenylethyl]-1H-pyrrolo[2,3-d]pyrimidin-4-amine ;[6-[4-[(4-Ethylpiperazin-1-yl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-((R)-1-phenylethyl)amine |
AEE788 (NVP-AEE788),EGFR和VEGFR抑制剂
AEE788 (NVP-AEE788) （订货以英文为准）
编号：A126830
CAS号：497839-62-0
分子式：C27H32N6
分子量：440.58
| 产品名称 | AEE788 (NVP-AEE788) |
| 中文名称 | AEE788 (NVP-AEE788),EGFR和VEGFR抑制剂 |
| CAS号 | 497839-62-0 |
| 分子式（M.F.） | C27H32N6 |
| 分子量（M.W.） | 440.58 |
| 储存条件 | -20°C储存 |
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