EG-011 | WASP activator | Probechem Biochemicals

Chemical Structure : EG-011

CAS No.: 2377113-41-0

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EG-011 (WASP activator EG-011, EG011)

货号: 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.

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10 mg	￥2580	In stock
25 mg	￥4880	In stock
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100 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	482.54
分子式	C28H26N4O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-(1-acryloylpiperidin-3-yl)-1-(4-phenoxybenzyl)pyrido[3,2-d]pyrimidine-2,4(1H,3H)-dione

参考文献

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.

EG-011 (WASP activator EG-011, EG011)

生物&药学活性

物理化学性质&存储条件

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EG-011 (WASP activator EG-011, EG011)

生物&药学活性

物理化学性质&存储条件

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