ZD-2767P
Based on 1 Customer Validation
ZD-2767P is a key prodrug in the antibody-directed enzyme prodrug therapy (ADEPT) system. The mechanism of action of ZD-2767Prelies entirely on the ADEPT strategy and proceeds in two steps: first, ZD2767C is administered, which locally enriches carboxypeptidase G2 at tumor sites; then, the prodrug ZD-2767P is administered, which is specifically recognized by the locally enriched carboxypeptidase G2, with its carbamate bond hydrolyzed to release the active drug ZD2767D. ZD-2767P can be used in research related to clear cell renal cell carcinoma, colorectal cancer and colon cancer.
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。
- CAS 番号: 156079-88-8
- 分子式: C16H20I2N2O6
- 分子量:590.15
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保管条件:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | IC50 |
47.2 μM
Compound: 1b
|
Cytotoxicity against colorectal tumor cell line LoVo 1 hour after incubation.
Cytotoxicity against colorectal tumor cell line LoVo 1 hour after incubation.
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[PMID: 8544182] |
体外実験
ZD-2767P (1 h incubation; 3 days post-wash culture) has low inherent cytotoxicity against LoVo colorectal tumor cells (IC50 = 47 ± 31 μM), but when cleaved by CPG2, releases a metabolite with potent cytotoxicity against these cells (IC50 = 0.32 ± 0.28 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nude mice (nu/nu: Alpk, outbred)[2]
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Dosage:3 × 70 mg/kg; 3 × 62 mg/kg; 3 × 52 mg/kg; 3 × 90 mg/kg; 3 × 90 mg/kg + 0.5 mg/kg ZD2767C
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Administration:i.p.; three hourly injections over a 2-hour period; administered 72 hours after ZD2767C
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Result:Induced complete macroscopic regression in 50% (22 of 39) of tumors, with tumors later reappearing in most cases.
Produced tumor growth delays of 33 days (3 × 70 mg/kg), 37 days (3 × 62 mg/kg), 32 days (3 × 52 mg/kg), 20 days (3 × 90 mg/kg), and 16 days (3 × 90 mg/kg with 0.5 mg/kg ZD2767C).
Caused 7-10% body-weight loss across doses.
Showed no antitumor activity when administered alone.
化学情報
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CAS 番号 156079-88-8
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性状 Solid
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分子量 590.15
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分子式 C16H20I2N2O6
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Color Light yellow to yellow
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(OC1=CC=C(N(CCI)CCI)C=C1)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (42.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6945 mL | 8.4724 mL | 16.9448 mL | 42.3621 mL |
| 5 mM | 0.3389 mL | 1.6945 mL | 3.3890 mL | 8.4724 mL | |
| 10 mM | 0.1694 mL | 0.8472 mL | 1.6945 mL | 4.2362 mL | |
| 15 mM | 0.1130 mL | 0.5648 mL | 1.1297 mL | 2.8241 mL | |
| 20 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL | 2.1181 mL | |
| 25 mM | 0.0678 mL | 0.3389 mL | 0.6778 mL | 1.6945 mL | |
| 30 mM | 0.0565 mL | 0.2824 mL | 0.5648 mL | 1.4121 mL | |
| 40 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0591 mL |