Agelastatin A
Agelastatin A ((-)-Agelastatin A; AglA), a tetracyclic alkaloid isolated from the sponge Agelas dendromorpha, induces apoptosis and arrests cells in the G2/M phase of the cell cycle, exhibiting antitumor activity.
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- CAS 番号: 152406-28-5
- 分子式: C12H13BrN4O3
- 分子量:341.16
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
0.46 μM
Compound: 1; AglA
|
Cytotoxicity against human A431 cells after 48 hrs by crystal violet staining based assay
Cytotoxicity against human A431 cells after 48 hrs by crystal violet staining based assay
|
[PMID: 26951751] |
| BXPC-3 | GI50 |
0.089 μg/mL
Compound: 82
|
Growth inhibition of human BXPC-3 cells assessed as reduction in cell viability measured after 3 days by CCK-8 assay
Growth inhibition of human BXPC-3 cells assessed as reduction in cell viability measured after 3 days by CCK-8 assay
|
[PMID: 38181652] |
| DU-145 | GI50 |
0.056 μg/mL
Compound: 82
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Growth inhibition of human DU-145 cells
Growth inhibition of human DU-145 cells
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[PMID: 38181652] |
| DU-145 | IC50 |
2.3 μM
Compound: 1, AA, (-)-Agelastatin A
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Cytotoxicity against human DU145 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay
Cytotoxicity against human DU145 cells assessed as inhibition of cell proliferation after 24 hrs by MTT assay
|
10.1039/C3MD00094J |
| FaDu | GI50 |
0.24 μg/mL
Compound: 82
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Growth inhibition of human FaDu cells
Growth inhibition of human FaDu cells
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[PMID: 38181652] |
| HeLa | EC50 |
0.11 μM
Compound: 1a
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Antitumor activity against human HeLa cells assessed as cell viability by MTT assay
Antitumor activity against human HeLa cells assessed as cell viability by MTT assay
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[PMID: 24673739] |
| HeLa | IC50 |
0.084 μM
Compound: 1; AglA
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Cytotoxicity against human HeLa cells after 24 hrs by [3H]-thymidine incorporation assay
Cytotoxicity against human HeLa cells after 24 hrs by [3H]-thymidine incorporation assay
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[PMID: 26951751] |
| JVM-2 | EC50 |
0.28 μM
Compound: 1a
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Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis
Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis
|
[PMID: 24673739] |
| KB | IC50 |
0.5 μg/mL
Compound: 1a
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Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
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[PMID: 24673739] |
| KM-20L2 | GI50 |
0.036 μg/mL
Compound: 82
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Growth inhibition of human KM-20L2 cells
Growth inhibition of human KM-20L2 cells
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[PMID: 38181652] |
| MCF7 | GI50 |
0.033 μg/mL
Compound: 82
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Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
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[PMID: 38181652] |
| NCI-H460 | GI50 |
0.036 μg/mL
Compound: 82
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Growth inhibition of human NCI-H460 cells
Growth inhibition of human NCI-H460 cells
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[PMID: 38181652] |
| P388 | ED50 |
0.052 μg/mL
Compound: 82
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Anticancer activity against mouse P388 cells assessed as inhibition of cell growth
Anticancer activity against mouse P388 cells assessed as inhibition of cell growth
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[PMID: 38181652] |
| Raji | IC50 |
0.14 μM
Compound: 1, AA, (-)-Agelastatin A
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Cytotoxicity against human Raji cells assessed as inhibition of cell proliferation after 3 days by coulter counter analysis
Cytotoxicity against human Raji cells assessed as inhibition of cell proliferation after 3 days by coulter counter analysis
|
10.1039/C3MD00094J |
| SF-268 | GI50 |
0.038 μg/mL
Compound: 82
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Growth inhibition of human SF-268 cells
Growth inhibition of human SF-268 cells
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[PMID: 38181652] |
| SJSA-1 | IC50 |
0.44 μM
Compound: 1; AglA
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Cytotoxicity against human SJSA1 cells after 48 hrs by crystal violet staining based assay
Cytotoxicity against human SJSA1 cells after 48 hrs by crystal violet staining based assay
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[PMID: 26951751] |
| SK-N-SH | GI50 |
0.042 μg/mL
Compound: 82
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Growth inhibition of human SK-N-SH cells
Growth inhibition of human SK-N-SH cells
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[PMID: 38181652] |
| SW-1736 | GI50 |
0.12 μg/mL
Compound: 82
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Growth inhibition of human SW-1736 cells
Growth inhibition of human SW-1736 cells
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[PMID: 38181652] |
Agelastatin A(0-2 μM, 48 h) has IC50 values of 67 nM, 708 nM, 1.05 μM, 278 nM and 1.11 μM on U-937, HeLa, A549, BT549 and IMR90 cells, respectively[1].
Agelastatin A(0-1 μM, 48 h) has IC50 values of 20, 74, 20, 138 and 187 nM on CEM, Jurkat, Daudi, HL-60 and CA46 cells, respectively[1].
Agelastatin A (0-150 nM, 16 h) can dose-dependently induce U-937 cell cycle arrest at G2/M[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Parameter/td> | intravenous (IV) | intraperitoneal (IP) |
| ACU | 1742 | 2946 |
| Cmax | 4.5 μM | 1.65 μM |
| Tmax | 2 min | 30 min |
| t1/2 | 4 min | 1 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 152406-28-5
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分子量 341.16
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分子式 C12H13BrN4O3
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SMILES
BrC(N1[C@@]2([H])[C@](N3)([H])[C@@]4([H])[C@@](C2)(N(C(N4)=O)C)O)=CC=C1C3=O
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別名
(-)-Agelastatin A; AglA
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Structure Classification
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Initial Source
A. dendromorpha
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Sunkyu Han, et al. Synthesis and anticancer activity of all known (-)-agelastatin alkaloids. J Org Chem. 2013 Dec 6;78(23):11970-84. [Content Brief]
[2]. E Paige Stout, et al. Potent fluorinated agelastatin analogues for chronic lymphocytic leukemia: design, synthesis, and pharmacokinetic studies. J Med Chem. 2014 Jun 26;57(12):5085-93. doi: 10.1021/jm4016922. Epub 2014 Jun. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Agelastatin A 関連分類
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