Astemizole
Astemizole is a potent anti-histamine compound that antagonizes the histamine H1-receptor with IC50 of 4 nM. It is also identified less potent at muscarinic acetylcholine receptors with Ki of 2.4 μM.
The histamine H1 receptor, a member of Rhodopsin-like G-protein-coupled receptors, is activated by the biogenic amine histamine and is expressed throughout the body, particularly in smooth muscles, on vascular endothelial cells, in the central nervous system, and in the heart.
Astemizole targets imperative proteins included in tumor movement, to be specific, either à-go-go 1 (Eag1) and Eag-related quality (Erg) potassium channels. Moreover, Eag1 is thought to be an imperative marker for a few distinct tumors. Astemizole hinders Eag1 and Erg channel action, and in cells communicating the Eag1 channel it diminishes tumor cell expansion in vitro and in vivo. It ought to be noticed that some cardiovascular reactions have been reported for astemizole in a couple of uncommon cases. Nevertheless, astemizole remains as an extremely encouraging hostile to malignancy apparatus on the grounds that it shows anti-proliferative mechanisms, may serve as the basis to synthesize new anti-cancer agents, and has been previously administered clinically. [1]
Reference:
1. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011 Mar;11(3):307-14.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 458.57 |
| Cas No. | 68844-77-9 |
| Formula | C28H31FN4O |
| Solubility | insoluble in H2O; ≥11.46 mg/mL in DMSO with gentle warming; ≥12.46 mg/mL in EtOH |
| Chemical Name | 1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine |
| SDF | Download SDF |
| Canonical SMILES | FC1=CC=C(C=C1)CN2C(NC3CCN(CCC(C=C4)=CC=C4OC)CC3)=NC5=CC=CC=C25 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Animal experiment:[1] | |
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Animal models |
Mice xenografted with the human breast cancer cell line T-47D and a primary breast cancer-derived cell culture (MBCDF) |
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Dosage form |
50 mg/kg/day Administered by oral route for 3 weeks |
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Applications |
Compared to untreated controls, astemizole and calcitriol significantly reduced, while the coadministration of both drugs further suppressed, tumor growth. In addition, the combined therapy significantly downregulated tumoral EAG1 and Ki-67 expression. Hence, in vivo dual targeting of the oncogenic EAG1 potassium channel by astemizole and calcitriol was able to enhance antineoplastic effects in breast tumors. |
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Note |
The technical data provided above is for reference only. |
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References: 1. García-Quiroz J, García-Becerra R, Santos-Martínez N, et al. In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumors. BMC Cancer, 2014, 14: 745. |
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Quality Control & MSDS
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Chemical structure
