Zoptarelin doxorubicin (AEZS-108; AN-152) 是一种混合抗癌剂，包括 Zoptarelin 和 Doxorubicin。Zoptarelin doxorubicin 可明显抑制肿瘤进展，在体外诱导细胞凋亡 (apoptosis)。Zoptarelin doxorubicin 已用于靶向LHRH受体表达肿瘤的研究。
| 生物活性 | Zoptarelin doxorubicin (AEZS-108; AN-152) is a hybrid anticancer agent, containing Zoptarelin andDoxorubicin. Zoptarelin doxorubicin has been used to research targeting tumors expressingLHRH receptors. Zoptarelin doxorubicin abolishes tumor progression and induces remarkableapoptosisin vitro[1]. |
| IC50& Target | Apoptosis, LHRH receptors[1] |
体外研究
(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].
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. |
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体内研究
(In Vivo) | Zoptarelin doxorubicin (AN-152) inhibits tumor growth in glioblastoma xenograft mice[1].
| Animal Model: | Female nude mice (injected in the flanks with 1×106glioblastoma 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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