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Chemical Structure : Targefrin
Catalog No.: 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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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.
| M.Wt | 1700.976 | |
| Formula | C85H116F3N19O15 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Carlo Baggio, et al. Journal of Medicinal Chemistry. November 4, 2022
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