EG-011 is a first-in-class, potent activator of Wiskott-Aldrich syndrome protein (WASP). EG-011 activates an autoinhibitory form of WASP through strong actin polymerization. EG-011 has selective anti-lymphoma activity.

Physicochemical Properties

Molecular Formula	C28H26N4O4
Molecular Weight	482.53
Exact Mass	482.195
CAS #	2377113-41-0
PubChem CID	139552342
Appearance	White to off-white solid powder
LogP	3.7
Hydrogen Bond Donor Count	0
Hydrogen Bond Acceptor Count	5
Rotatable Bond Count	6
Heavy Atom Count	36
Complexity	820
Defined Atom Stereocenter Count	0
SMILES	C1(CCCN(C(=O)C=C)C1)N1C(=O)C2N=CC=CC=2N(CC2C=CC(OC3C=CC=CC=3)=CC=2)C1=O
InChi Key	JBKILBGEQHFIOB-UHFFFAOYSA-N
InChi Code	InChI=1S/C28H26N4O4/c1-2-25(33)30-17-7-8-21(19-30)32-27(34)26-24(11-6-16-29-26)31(28(32)35)18-20-12-14-23(15-13-20)36-22-9-4-3-5-10-22/h2-6,9-16,21H,1,7-8,17-19H2
Chemical Name	1-[(4-phenoxyphenyl)methyl]-3-(1-prop-2-enoylpiperidin-3-yl)pyrido[3,2-d]pyrimidine-2,4-dione
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	In lymphoma cell lines (OCI-LY-19 and REC1), EG-011 (500 nM, 2 μM; 72 hours) increases cell mortality in a dose-dependent manner (20–55%). Normal PBMC are not cytotoxic to EG-011 (1, 10 mM; for 24, 48 hours) [1]. Actin polymerization in EG-011-sensitive (VL51) but not resistant (Z138) cell lines is increased by EG-011 (500 nM, 5 μM; 24 hours) at two concentrations [2].
ln Vivo	In female NOD-SCID mice carrying MCL REC-1 cells, EG-011 (200 mg/kg; i.p.; 5 days per week) slows tumor growth (days 6, 7, 9). At weight, the tumor was 2.2 times smaller than the control (P<0.001)[1].
References	[1]. 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]. 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]. 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.

Solubility Data

Solubility (In Vitro)

DMSO : 125 mg/mL (259.05 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0724 mL	10.3621 mL	20.7241 mL
	5 mM	0.4145 mL	2.0724 mL	4.1448 mL
	10 mM	0.2072 mL	1.0362 mL	2.0724 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.