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Chemical Structure : EG-011
CAS No.: 2377113-41-0
Catalog No.: PC-49819Not For Human Use, Lab Use Only.
EG-011 (WASP activator EG-011, EG011) is a first-in-class, small molecule activator of the auto-inhibited form of Wiskott-Aldrich syndrome protein (WASp) with selective anti-tumor activity in lymphomas.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $258 | In stock | |
| 25 mg | $488 | In stock | |
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EG-011 (WASP activator EG-011, EG011) is a first-in-class, small molecule activator of the auto-inhibited form of Wiskott-Aldrich syndrome protein (WASp) with selective anti-tumor activity in lymphomas.
The anti-tumor activity of EG-011 was maintained in the resistant cell line derived from the MZL VL51 with secondary resistance to ibrutinib (IC50: 500 nM in both parental and resistant), while it was higher in the MZL model with resistance to PI3Kdelta inhibitor derived from VL51 (IC50: 100 nM).
The copanlisib-resistant MZL VL51 (IC50: 2 μM) and Karpas1718 idelalisib-resistant (5 nM) showed a slightly decreased sensitivity to EG-011 (Karpas1718 parental, IC50: 1 nM).
The AMO-1 carfilzomib resistant cell line showed an IC50 to EG-011 treatment that was more than 20 times lower that the carfilzomib sensitive parental cell line (IC50: 250 nM vs 6 μM).
EG-011 is a novel small molecule with in vitro and in vivo anti-tumor activity against lymphoma and acute leukemias, but, at least so far, no activity in solid tumor models (Gaudio et al AACR 2019).
| M.Wt | 482.54 | |
| Formula | C28H26N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
3-(1-acryloylpiperidin-3-yl)-1-(4-phenoxybenzyl)pyrido[3,2-d]pyrimidine-2,4(1H,3H)-dione |
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1. Eugenio Gaudio, et al. Cancer Res (2019) 79 (13_Supplement): 4796.
2. PCT/EP2018/057678
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. Eur J Cancer, VOLUME 174, SUPPLEMENT 1, S107, OCTOBER 2022.
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