Targefrin

Chemical Structure : Targefrin

CAS No.: 3031514-44-7

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货号: PC-49438Not For Human Use, Lab Use Only.

Targefrin is a potent, selective antagonist targeting ligand binding domain of receptor tyrosine kinase EphA2 (EphA2-LBD), binds to EphA2-LBD with Kd of 21 nM (ITC) and shows IC50 value of 10.8 nM in biochemical assays.

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1 mg	￥2980	In stock
5 mg	￥5980	In stock
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25 mg		Get quote

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生物&药学活性

Targefrin is a potent, selective antagonist targeting ligand binding domain of receptor tyrosine kinase EphA2 (EphA2-LBD), binds to EphA2-LBD with Kd of 21 nM (ITC) and shows IC50 value of 10.8 nM in biochemical assays.
Targefrin displays no significant affinity against the LBDs of EphA3 and EphA4.
Targefrin effectively antagonized EphA2 degradation induced by the potent ephrinA1-Fc ligand in BxPC3 pancreatic cancer cells with EC50 of 1.6 uM.

物理化学性质&存储条件

分子量	1700.976
分子式	C85H116F3N19O15
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-3-((S)-1-((2S,5S,8S,11S)-11-(4-aminobenzyl)-8-isobutyl-5-methyl-4,7,10,13-tetraoxo-14-(piperazin-1-yl)-2-((2'-(trifluoromethyl)-[1,1'-biphenyl]-4-yl)methyl)-3,6,9,12-tetraazatetradecanoyl)pyrrolidine-2-carboxamido)-4-(((S)-1-(((S)-2-((S)-2-(((S)-1-(((S)-1-((S)-2-carbamoylpyrrolidin-1-yl)-5-guanidino-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)carbamoyl)pyrrolidin-1-yl)-1-cyclohexyl-2-oxoethyl)amino)-1-oxopropan-2-yl)amino)-4-oxobutanoic acid

参考文献

1. Carlo Baggio, et al. Journal of Medicinal Chemistry. November 4, 2022

Targefrin

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Targefrin

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