NAMPT inhibitor-linker 2
Based on 1 Customer Validation
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
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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: 2241014-82-2
- 分子式: C34H33FN6O5
- 分子量:624.66
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Drug-Linker Conjugates for ADC 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
IC50 & Target
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Traditional Cytotoxic Agents |
体外実験
ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively[1].
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GIST-T1 cells
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Concentration:0.1 pM-10 nM
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Incubation Time:144 hours
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Result:Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.
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:Female scid-beige (SCID bg) mice[1]
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Dosage:20 mg/kg
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Administration:A single intravenous injection (i.v.) for 28 days
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Result:Significantly inhibited the growth of tumor in mice.
化学情報
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CAS 番号 2241014-82-2
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性状 Solid
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分子量 624.66
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分子式 C34H33FN6O5
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Color Off-white to light yellow
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SMILES
FC1=CC(NC([C@@H]2[C@H](C2)C3=CN=CC=C3)=O)=CC=C1CNC(C4=CC=C(N5CCN(C(CCN6C(C=CC6=O)=O)=O)CC5)C=C4)=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
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (80.04 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. 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. 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)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (271 KB)
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SDS (251 KB)
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- Portuguese - PT (251 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. 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 |
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| DMSO | 1 mM | 1.6009 mL | 8.0044 mL | 16.0087 mL | 40.0218 mL |
| 5 mM | 0.3202 mL | 1.6009 mL | 3.2017 mL | 8.0044 mL | |
| 10 mM | 0.1601 mL | 0.8004 mL | 1.6009 mL | 4.0022 mL | |
| 15 mM | 0.1067 mL | 0.5336 mL | 1.0672 mL | 2.6681 mL | |
| 20 mM | 0.0800 mL | 0.4002 mL | 0.8004 mL | 2.0011 mL | |
| 25 mM | 0.0640 mL | 0.3202 mL | 0.6403 mL | 1.6009 mL | |
| 30 mM | 0.0534 mL | 0.2668 mL | 0.5336 mL | 1.3341 mL | |
| 40 mM | 0.0400 mL | 0.2001 mL | 0.4002 mL | 1.0005 mL | |
| 50 mM | 0.0320 mL | 0.1601 mL | 0.3202 mL | 0.8004 mL | |
| 60 mM | 0.0267 mL | 0.1334 mL | 0.2668 mL | 0.6670 mL | |
| 80 mM | 0.0200 mL | 0.1001 mL | 0.2001 mL | 0.5003 mL |
NAMPT inhibitor-linker 2 関連分類
HY-112616 関連分類
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