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Targefrin

Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines[1].

Product Specifications

CAS Number

[3031514-44-7]

UNSPSC

12352209

Target

Ephrin Receptor

Type

Peptides

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/targefrin.html

Purity

99.80

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

C[C@H](NC([C@@H](NC([C@@H](NC(CN1CCNCC1)=O)CC2=CC=C(N)C=C2)=O)CC(C)C)=O)C(N[C@H](C(N3CCC[C@H]3C(N[C@@H](CC(O)=O)C(N[C@H](C(N[C@@H](C4CCCCC4)C(N(CCC5)[C@@H]5C(N[C@@H](CC6=CC=CC=C6)C(N[C@@H](CCCNC(N)=N)C(N7CCC[C@H]7C(N)=O)=O)=O)=O)=O)=O)C)=O)=O)=O)CC8=CC=C(C=C8)C9=CC=CC=C9C(F)(F)F)=O

Molecular Formula

C85H116F3N19O15

Molecular Weight

1700.94

References & Citations

[1]Baggio C, Udompholkul P, Gambini L, Pellecchia M. Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2. J Med Chem. 2022 Nov 4.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture)

Scientific Category

Peptides

Clinical Information

No Development Reported

Available Sizes

Curated Selection

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