1. Antibody-drug Conjugate/ADC Related GPCR/G Protein
  2. Peptide-Drug Conjugates (PDCs) GnRH Receptor
  3. Zoptarelin doxorubicin

Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro.

For research use only. We do not sell to patients.

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Zoptarelin doxorubicin

Zoptarelin doxorubicin Chemical Structure

CAS No. : 139570-93-7

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Description

Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin and Doxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressing LHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkable apoptosis in vitro[1].

IC50 & Target

Apoptosis, LHRH receptors[1]

In Vitro

Zoptarelin doxorubicin (AN-152) inhibits almost 70 % of glioblastoma cell growth, increases almost 250% apoptosis and causes a greater increase in calcein retention[1].
Zoptarelin doxorubicin (AN-152) up-regulates the tumor suppressor and pro-apoptotic p53, and inhibits the expression of the primordial, neuroectodermal stem cell marker, nestin[1].

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

Cell Proliferation Assay[1]

Cell Line: U-87 MG
Concentration: 100 nM
Incubation Time: 48 h
Result: Brought about an almost 70 % inhibition of tumor cell growth.

Apoptosis Analysis[1]

Cell Line: U-87 MG
Concentration: 100 nM
Incubation Time: 48 h
Result: Increased almost 250 % apoptosis.

Western Blot Analysis[1]

Cell Line: U-87 MG
Concentration: 100 nM
Incubation Time: 24 h
Result: Did not induce any down-regulation of LHRH-R.
Inhibited the expression of the primordial, neuroectodermal stem cell marker, nestin.
Up-regulated the tumor suppressor and pro-apoptotic p53.
In Vivo

Zoptarelin doxorubicin (AN-152) inhibits tumor growth in glioblastoma xenograft mice[1].

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

Animal Model: Female nude mice (injected in the flanks with 1×106 glioblastoma U-87 MG cells)[1]
Dosage: 413 nM/20g
Administration: i.v.; once weekly; for 6 weeks
Result: Significantly inhibited tumor growth compared to the control.
Clinical Trial
Molecular Weight

1893.01

Formula

C91H117N19O26

CAS No.
Appearance

Solid

Color

Orange to red

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture and light

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (26.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5283 mL 2.6413 mL 5.2826 mL
5 mM 0.1057 mL 0.5283 mL 1.0565 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
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 and light). 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
H2O 1 mM 0.5283 mL 2.6413 mL 5.2826 mL 13.2065 mL
5 mM 0.1057 mL 0.5283 mL 1.0565 mL 2.6413 mL
10 mM 0.0528 mL 0.2641 mL 0.5283 mL 1.3206 mL
15 mM 0.0352 mL 0.1761 mL 0.3522 mL 0.8804 mL
20 mM 0.0264 mL 0.1321 mL 0.2641 mL 0.6603 mL
25 mM 0.0211 mL 0.1057 mL 0.2113 mL 0.5283 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Product Name:
Zoptarelin doxorubicin
Cat. No.:
HY-16532
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