| Identification | Back Directory | [Name]
EG-011 | [CAS]
2377113-41-0 | [Synonyms]
EG-011
Pyrido[3,2-d]pyrimidine-2,4(1H,3H)-dione, 3-[1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-1-[(4-phenoxyphenyl)methyl]- | [Molecular Formula]
C28H26N4O4 | [MOL File]
2377113-41-0.mol | [Molecular Weight]
482.53 |
| Chemical Properties | Back Directory | [Boiling point ]
710.1±70.0 °C(Predicted) | [density ]
1.312±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.25±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
EG-011 (200 mg/kg; i.p.; 5 days per week) delays tumor growth (Day 6, Day 7, Day 9) and tumor weight in female NOD-SCID mice with the MCL REC-1 cell line. EG-011-treated tumors are 2.2-fold smaller than controls (P<0.001)[1].
| [References]
[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. |
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