7-メチルグアニン
Based on 1 Customer Validation
7-Methylguanine is an orally active and competitive PARP-1 inhibitor with a Ki value of 61 μM. 7-Methylguanine is a metabolite of nucleic acids. 7-Methylguanine has anticancer activity against uterine sarcoma and colon adenocarcinoma. 7-Methylguanine is used as a probe for protein-DNA interactions.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.97%
- CAS 番号: 578-76-7
- 分子式: C6H7N5O
- 分子量:165.15
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Endogenous Metabolite アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
|
Human Endogenous Metabolite |
PARP-1 61 μM (Ki) |
体外実験
7-Methylguanine (0-200 μM) inhibits PARP1 enzymatic activity in a dose-dependent manner[1].
7-Methylguanine is a competitive PARP-1 inhibitor with a Ki value of 61 μM[2].
7-Methylguanine (0-450 μM) inhibits the dissociation of the PARP-1-DNA complex due to suppression of PARP-1 catalytic activity[2].
7-Methylguanine (0.02-0.2 mg/mL; 24 h) does not produce DNA damage in immortalized human kidney epithelial cells (NKE-hTERT)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
7-Methylguanine (50 mg/kg; i.g.; 3 times per week) effectively penetrates tumor tissue and suppresses colon adenocarcinoma growth in BALB/c mice with transplanted Akatol tumor[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CBA, BALB/c, C57BL/6 mice (6-week-old); toxicology study and carcinogenicity study[3]
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Dosage:50 mg/kg, 200 mg/kg, 600 mg/kg
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Administration:Intragastric administration, 3 times per week for 4 weeks (for 50 mg/kg group), 3 times per week for 1 week (for 200 mg/kg group), single dose (for 600 mg/kg group)
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Result:Exerted no adverse effects or changes in morphology (at 50 mg/kg for 3 times per week up to 4 weeks).
Caused some lymphoid infiltrates in lungs, liver and spleen, and focal lymphoid hyperplasia in intestines in CBA mice (at 600 mg/kg single dose).
Did not induce mutations or structural chromosomal abnormalities, and had no blastomogenic activity.
Significantly inhibited tumor growth in CBA mice with uterine sarcoma US-322 (at 50 mg/kg 3 times per week).
Had an antitumor effect in CBA mice with cervical squamous cell carcinoma RShM-5 (alone for 1 week).
Inhibited tumor growth in combination with Cisplatin (HY-17394) within a week after inoculation.
化学情報
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CAS 番号 578-76-7
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性状 Solid
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分子量 165.15
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分子式 C6H7N5O
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Color White to light yellow
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SMILES
O=C1NC(N)=NC2=C1N(C)C=N2
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別名
7-Methylguanine
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
1 M NaOH : ≥ 100 mg/mL (605.51 mM)
H2O : 4.72 mg/mL (28.58 mM; ultrasonic and adjust pH to 11 with 1 M NaOH)
* "≥" means soluble, but saturation unknown.
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 (protect from 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.
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 (protect from 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kurgina TA, et al. Inhibitory Effects of 7-Methylguanine and Its Metabolite 8-Hydroxy-7-Methylguanine on Human Poly(ADP-Ribose) Polymerase 1. Biochemistry (Mosc). 2022 Aug;87(8):823-831. [Content Brief]
[2]. Nilov D, et al. Molecular Mechanisms of PARP-1 Inhibitor 7-Methylguanine. Int J Mol Sci. 2020 Mar 20;21(6):2159. [Content Brief]
[3]. Kirsanov K, et al. Toxicological Properties of 7-Methylguanine, and Preliminary Data on its Anticancer Activity. Front Pharmacol. 2022 Jul 6;13:842316. [Content Brief]
[4]. Gaubatz JW, et al. Introduction, distribution, and removal of 7-methylguanine in different liver chromatin fractions of young and old mice. Mutat Res. 1997 Apr 14;375(1):25-35. [Content Brief]
[5]. Kirsanov K, et al. 7-Methylguanine Inhibits Colon Cancer Growth in Vivo. Acta Naturae. 2024 Apr-Jun;16(2):50-52. [Content Brief]
[6]. Lee S, et al. Synthesis and structure of duplex DNA containing the genotoxic nucleobase lesion N7-methylguanine. J Am Chem Soc. 2008 Sep 3;130(35):11570-1. [Content Brief]
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 (protect from 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 M NaOH | 1 mM | 6.0551 mL | 30.2755 mL | 60.5510 mL | 151.3775 mL |
| 5 mM | 1.2110 mL | 6.0551 mL | 12.1102 mL | 30.2755 mL | |
| 10 mM | 0.6055 mL | 3.0276 mL | 6.0551 mL | 15.1378 mL | |
| 15 mM | 0.4037 mL | 2.0184 mL | 4.0367 mL | 10.0918 mL | |
| 20 mM | 0.3028 mL | 1.5138 mL | 3.0276 mL | 7.5689 mL | |
| 25 mM | 0.2422 mL | 1.2110 mL | 2.4220 mL | 6.0551 mL | |
| 1 M NaOH | 30 mM | 0.2018 mL | 1.0092 mL | 2.0184 mL | 5.0459 mL |
| 40 mM | 0.1514 mL | 0.7569 mL | 1.5138 mL | 3.7844 mL | |
| 50 mM | 0.1211 mL | 0.6055 mL | 1.2110 mL | 3.0276 mL | |
| 60 mM | 0.1009 mL | 0.5046 mL | 1.0092 mL | 2.5230 mL | |
| 80 mM | 0.0757 mL | 0.3784 mL | 0.7569 mL | 1.8922 mL | |
| 100 mM | 0.0606 mL | 0.3028 mL | 0.6055 mL | 1.5138 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.
7-Methylguanine 関連分類
HY-113352 関連分類
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