EVT801 | VEGFR-3 inhibitor | Probechem Biochemicals

Chemical Structure : EVT801

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EVT801 (EVT-801, EVT 801)

货号: PC-20338Not For Human Use, Lab Use Only.

EVT801 (EVT 801) is a potent, selective VEGFR-3 inhibitor with biochemical IC50 of 11 nM, inhibits cellular VEGFR-3 autophosphorylation with IC50 of 39 nM.

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生物&药学活性

EVT801 (EVT 801) is a potent, selective VEGFR-3 inhibitor with biochemical IC50 of 11 nM, inhibits cellular VEGFR-3 autophosphorylation with IC50 of 39 nM.
EVT801 displays 30-fold and 50-fold selectivity over VEGFR-2 and VEGFR-1 in cellular assays, respectively.
EVT801 potently inhibits VEGFR-3 autophosphorylation in various mammalian species, with an IC50 in cellular assays ranging from 151 nM for the mouse receptor to 32 nM for the monkey protein.
EVT801 undergoes O-demethylation in the cell, giving rise to the active metabolite SAR401849, which is as potent and selective as EVT801.
EVT801 strongly inhibited VEGF-C–induced ERK1/2 phosphorylation with an IC50 of 13 nM in hLMVECs.
EVT801 inhibited the induction of hLMVEC proliferation in a dose-dependent manner with an IC50 of 15 nmol/L for VEGF-C, 8 nmol/L for VEGF-D, and 155 nmol/L for VEGF-A, and a maximum inhibition of 74%, 100%, and 65%, respectively.
EVT801 reduced ERK phosphorylation induced by VEGF-C and VEGF-D better than pazopanib in NCI-H1703 cells.
EVT801(30 mg/kg twice per day, oral) showed a significant inhibition of tumor growth in NCI-H1703 tumor xenografts, blocked hypoxia-driven immunosuppression and enhances ICT efficacy.

物理化学性质&存储条件

分子量	367.41
分子式	C19H21N5O3
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	2-amino-1-ethyl-7-(3-hydroxy-4-methoxy-3-methylbut-1-yn-1-yl)-3-(1H-imidazol-2-yl)-1,8-naphthyridin-4(1H)-one

参考文献

1. Michael R Paillasse, et al. Cancer Res Commun. 2022 Nov 29;2(11):1504-1519.

EVT801 (EVT-801, EVT 801)

生物&药学活性

物理化学性质&存储条件

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EVT801 (EVT-801, EVT 801)

生物&药学活性

物理化学性质&存储条件

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