AEE788 is a multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC 50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. [1] .

AEE788 对一系列 EGFR 和 ErbB2 过表达细胞系 (包括 EGFRvIII 依赖性细胞系) 具有抗增殖活性，并抑制表皮生长因子和 VEGF 刺激的人脐静脉内皮细胞的增殖 [1]。 AEE788 处理皮肤 SCC 细胞导致 EGFR 和 VEGFR-2 磷酸化的剂量依赖性抑制、生长抑制并诱导细胞凋亡 [2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. AEE788 有效抑制肿瘤中生长因子诱导的 EGFR 和 ErbB2 磷酸化，该抑制活性超过 72 小时。 …

AEE788 is an orally active, reversible, small-molecule, multi-targeted kinase inhibitor with potent inhibitory activity against the ErbB and VEGF receptor family of tyrosine kinases. It has an IC50 of less than 100 nM against p-EGFR, p-ErbB2, and p-KDR (VEGFR2).

2016年10月20日 · Regulates both osteogenesis and postnatal bone mineralization by osteoblasts. Promotes apoptosis in chondrocytes, but can also promote cancer cell proliferation. Required for normal development of the inner ear.

2004年7月15日 · 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 on the isolated enzyme level and in cellular systems.

AEE788 is a 6- {4- [ (4-ethylpiperazin-1-yl)methyl]phenyl}-N- (1-phenylethyl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine which adopts an R-configuration. It is a potent inhibitor of human EGFR, VEGFR and HER2 receptor tyrosine kinases and exhibits anticancer and antiangiogenic activity.

AEE788 (NVP-AEE788) 是一种高效的 EGFR 、 VEGFR 和 HER2/ErbB2 抑制剂，其对 EGFR 和 ErbB2 的 IC50 值分别为 2 nM 和 6 nM， AEE788 也抑制 Flt-1 、 KDR 、 c-Src 和 c-Abl，其作用得 IC 50 值为 50-80 nM。 AEE788 抑制 EGFR 和 Akt 的磷酸化，抑制肿瘤细胞增殖。 产品性质. CAS 号（CAS NO.） 运输和保存方法. 冰袋运输。 粉末直接保存于 -20℃， 有效期 3 年。 溶于 DMSO。 建议分装后 -20℃ 避 光保存，避免反复冻融。 注意事项. 1） 为了您的安全和健 …

Purpose: Vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) play a significant role in glioblastoma angiogenesis and proliferation, making tyrosine kinase (TK) receptors logical targets for treatment. We evaluated AEE788, a reversible TK inhibitor that inhibits EGFR and VEGFR, in recurrent glioblastoma patients.

aee-788是由诺华制药研发的一种小分子药物，是一种her2拮抗剂、egfr拮抗剂和vegfr2拮抗剂。 目前该药物最高研发阶段为无进展，用于治疗脑癌、中枢神经系统肿瘤和胶质母细胞瘤。