1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. 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.

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Targefrin Chemical Structure

Targefrin Chemical Structure

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Description

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].

In Vitro

Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells[1].
Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: BxPC3 cells (starved for 1 h and pre-treated with Targefrin for 20 min, followed by a combination treatment with 2 μg/mL ephrinA1-Fc for 3 h)
Concentration: 0.025, 0.25, 0.5, 1, 2.5, 5, 7.5 and 10 μM
Incubation Time: 20 min
Result: Effectively antagonized EphA2 degradation induced by the potent ephrinA1-Fc ligand, with an approximate EC50 of ~1.6 μM.

Cell Migration Assay [1]

Cell Line: BxPC3 cells
Concentration: 2, 4, 5 and 10 μM
Incubation Time: 24 h
Result: Significantly inhibited pancreatic cancer cell migration.
In Vivo

Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated with Paclitaxel[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male nu/nu mice (injected with MIA PaCa-2 cells)[1]
Dosage: 50 mg/kg
Administration: i.v.; at day 1, 4, 8, 11 and 15
Result: Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group.
Animal Model: Balb/C mice[1]
Dosage: 50 mg/kg
Administration: IV via tail vein; single dosage
Result: Cmax ~650 ng/mL after 2 hours from the injection; estimated t1/2 ~15 hr.
Molecular Weight

1700.94

Formula

C85H116F3N19O15

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Targefrin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Targefrin
Cat. No.:
HY-P3717
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