2. Protein Tyrosine Kinase/RTK
  3. Ephrin Receptor
  4. 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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Custom Peptide Synthesis

Targefrin Chemical Structure

Targefrin Chemical Structure

CAS No. : 3031514-44-7

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5 mg USD 900 In-stock
10 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

Targefrin Related Antibodies

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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.

Targefrin Related Antibodies

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
CAS No.
Appearance

Solid

Color

White to off-white

Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (58.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5879 mL 2.9396 mL 5.8791 mL
5 mM 0.1176 mL 0.5879 mL 1.1758 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.5879 mL 2.9396 mL 5.8791 mL 14.6978 mL
5 mM 0.1176 mL 0.5879 mL 1.1758 mL 2.9396 mL
10 mM 0.0588 mL 0.2940 mL 0.5879 mL 1.4698 mL
15 mM 0.0392 mL 0.1960 mL 0.3919 mL 0.9799 mL
20 mM 0.0294 mL 0.1470 mL 0.2940 mL 0.7349 mL
25 mM 0.0235 mL 0.1176 mL 0.2352 mL 0.5879 mL
30 mM 0.0196 mL 0.0980 mL 0.1960 mL 0.4899 mL
40 mM 0.0147 mL 0.0735 mL 0.1470 mL 0.3674 mL
50 mM 0.0118 mL 0.0588 mL 0.1176 mL 0.2940 mL
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Targefrin Related Classifications

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.

Keywords:

Targefrin3031514-44-7Ephrin ReceptorEphA2pancreatic cancerInhibitorinhibitorinhibit

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