1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor
  3. UniPR129

UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy.

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UniPR129

UniPR129 Chemische Struktur

CAS. Nr. : 1639159-47-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Beschreibung

UniPR129 is a potent and orally active Eph/ephrin antagonist. UniPR129 can inhibit EphA2-ephrin-A1 interaction with an IC50 of 945 nM and a Ki of 370 nM. UniPR129 can inhibit angiogenesis and show antitumor and neuroprotective effect. UniPR129 can be used for the researches of cancer and neurological disease, such as colorectal cancer and optic neuropathy[1][2][3][4].

IC50 & Target[4]

EphA8

0.84 μM (IC50)

EphA2

1.12 μM (IC50)

EphA7

1.24 μM (IC50)

EphA1

1.39 μM (IC50)

EphA3

1.43 μM (IC50)

EphA6

1.53 μM (IC50)

EphA5

1.57 μM (IC50)

EphA4

1.58 μM (IC50)

EphB4

2.60 μM (IC50)

EphB1

2.75 μM (IC50)

EphB2

2.96 μM (IC50)

EphB5

3.01 μM (IC50)

EphB3

3.74 μM (IC50)

In Vitro

UniPR129 (1.5-25 μM, 20 mins) inhibits EphA2 activation in PC3 cells[1].
UniPR129 (6-50 μM, 2 h) does not show any toxic effect in PC3 cells[1].
UniPR129 (1.56-12.5, 20 mins) inhibits PC3 cells retraction[1].
UniPR129 (1.5-25, 15 h) inhibits angiogenesis in HUVECs[1].
UniPR129 (50 μM) shows neuroprotection in retinas isolated from optic nerve crush (ONC) injury mices model[3].

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

Immunofluorescence[1]

Cell Line: PC3 cells
Concentration: 1.56, 3.12, 6.25 and 12.5 μM
Incubation Time: 20 mins
Result: Inhibited the rounding effect of ephrin-A1-Fc
In Vivo

UniPR129 (30 mg/kg, p.o., every other day for 8 weeks) can slow down the tumor development in APC min/J mice [2].

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

Animal Model: APC min/J mice[2]
Dosage: 30 mg/kg
Administration: Orally administration, every other day for 8 weeks
Result: Reduced the formation of adenomas in the ileum of 1.6 times.
Reduced tumor volume.
Molekulargewicht

576.81

Formel

C36H52N2O4

CAS. Nr.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(N[C@H](CC(O)=O)CC3=CNC4=CC=CC=C34)=O)([H])[C@@]5([H])[C@]([C@@]6([C@](C[C@H](O)CC6)([H])CC5)C)([H])CC1

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 33.33 mg/mL (57.78 mM; ultrasonic and warming and heat to 60°C; 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 1.7337 mL 8.6684 mL 17.3367 mL
5 mM 0.3467 mL 1.7337 mL 3.4673 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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. 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 1.7337 mL 8.6684 mL 17.3367 mL 43.3418 mL
5 mM 0.3467 mL 1.7337 mL 3.4673 mL 8.6684 mL
10 mM 0.1734 mL 0.8668 mL 1.7337 mL 4.3342 mL
15 mM 0.1156 mL 0.5779 mL 1.1558 mL 2.8895 mL
20 mM 0.0867 mL 0.4334 mL 0.8668 mL 2.1671 mL
25 mM 0.0693 mL 0.3467 mL 0.6935 mL 1.7337 mL
30 mM 0.0578 mL 0.2889 mL 0.5779 mL 1.4447 mL
40 mM 0.0433 mL 0.2167 mL 0.4334 mL 1.0835 mL
50 mM 0.0347 mL 0.1734 mL 0.3467 mL 0.8668 mL
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  • 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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