| Bioactivity | EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas[1][2][3]. | |||||||||
| Invitro | EG-011 (500 nM, 2 μM; 72 小时) 在淋巴瘤细胞系 (OCI-LY-19 和 REC1) 中引起剂量依赖性细胞死亡增加 (20-55%)。EG-011 (1, 10 mM; for 24, 48 小时) 对正常的 PBMC 没有细胞毒性[1]。 EG-011 (500 nM, 5 μM; 24 小时) 导致 EG-011 敏感 (VL51) 而不是耐药 (Z138) 细胞系在 4、8 和 24 小时两种浓度下的肌动蛋白聚合增加[2] 。 | |||||||||
| In Vivo | EG-011 (200 mg/kg; 腹腔注射; 每周 5 天) 延迟带有 MCL REC-1 细胞的雌性 NOD-SCID 小鼠的肿瘤生长 (第 6 天、第 7 天、第 9 天) 和肿瘤重量，肿瘤比对照小 2.2 倍 (P<0.001)[1]。 | |||||||||
| Name | EG-011 | |||||||||
| CAS | 2377113-41-0 | |||||||||
| Formula | C28H26N4O4 | |||||||||
| Molar Mass | 482.53 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. E. Gaudio, et al. EG-011 IS A NOVEL SMALL MOLECULE WITH IN VITRO AND IN VIVOANTI-TUMOR ACTIVITY AGAINST LYMPHOMA. Hematological OncologyVolume 37: 15th International Conference on Malignant Lymphoma Palazzo dei Congressi, Lugano, Switzerland, 18-22 June, 2019. [2]. Filippo Spriano, et al. Abstract 1817: EG-011 is a first-in-class Wiskott-Aldrich syndrome protein (WASp) activator with anti-tumor activity. Cancer Res (2022) 82 (12_Supplement): 1817. [3]. F. Spriano, et al. The first-in-class WASP activator EG-011 is active in lymphoma and multiple myeloma cell lines resistant to FDA approved compounds. European Journal of Cancer 174S1 (2022) S3-S128. |