Zefamenib
Based on 1 Customer Validation
Zefamenib (BN-104) is an effective selective brain membrane protein inhibitor with oral activity, and it's also a Menin inhibitor, it can block the Menin-MLL interaction and leads to the degradation of Menin protein. Zefamenib is a weak hERG inhibitor, with an IC50 greater than 100 μM. Zefamenib has anti-tumor activity and can be used in cancer research, such as for acute myeloid leukemia.
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: 99.95%
- CAS 番号: 2938995-50-5
- 分子式: C31H35FN8O2
- 分子量:570.66
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保管条件:Powder -20°C, 3 years , 4°C, 2 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
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Epigenetics Compound Library
HY-L005
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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Clinical Compound Library
HY-L026
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Drug Repurposing Compound Library
HY-L035
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Reprogramming Compound Library
HY-L039
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Orally Active Compound Library
HY-L061
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Blood Cancer Compound Library
HY-L079
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Neurodegenerative Disease-related Compound Library
HY-L086
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Protein-protein Interaction Inhibitor Library
HY-L109
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Potassium Channel Compound Library
HY-L119
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Ion Channel Compound Library
HY-L166
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
生物活性
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hERG >100 μM (IC50) |
Zefamenib (BN-104) inhibits the proliferation of leukemia cells, with IC50 values of: MV-4-11 AF4 fusion (3.5 nM); MOLM13 AF9 fusion (12 nM); OCI-AML3 NPM1 mutant (11 nM)[1].
Zefamenib (10 μM, 0-24 h) causes degradation of Menin protein in MV-4-11 cells [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11, MOLM13, OCI-AML3
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:
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Result:Inhibited cell proliferation.
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Cell Line:MV-4-11
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Concentration:10 μM
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Incubation Time:2, 4, 6, 8, 24 h
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Result:Decreased expression of Menin protein.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MV-4-11 xenograft mouse model[1]
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Dosage:0, 10, 30, 60 mg/kg; twice a day; 21 days
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Administration:Oral
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Result:Inhibited tumor proliferation.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2938995-50-5
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性状 Solid
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分子量 570.66
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分子式 C31H35FN8O2
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Color White to off-white
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SMILES
O=C([C@@H]1[C@]2([H])[C@](CCC2)([H])CN1)N3CCC4(CC3)CN(C5=NC=NN=C5OC6=C(C7=CN=CN=C7C8CC8)C=C(C=C6)F)C4
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別名
BN-104; BNM-1192; Menin-MLL inhibitor 27
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (175.24 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)
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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.38 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 (280 KB)
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SDS (254 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7524 mL | 8.7618 mL | 17.5236 mL | 43.8089 mL |
| 5 mM | 0.3505 mL | 1.7524 mL | 3.5047 mL | 8.7618 mL | |
| 10 mM | 0.1752 mL | 0.8762 mL | 1.7524 mL | 4.3809 mL | |
| 15 mM | 0.1168 mL | 0.5841 mL | 1.1682 mL | 2.9206 mL | |
| 20 mM | 0.0876 mL | 0.4381 mL | 0.8762 mL | 2.1904 mL | |
| 25 mM | 0.0701 mL | 0.3505 mL | 0.7009 mL | 1.7524 mL | |
| 30 mM | 0.0584 mL | 0.2921 mL | 0.5841 mL | 1.4603 mL | |
| 40 mM | 0.0438 mL | 0.2190 mL | 0.4381 mL | 1.0952 mL | |
| 50 mM | 0.0350 mL | 0.1752 mL | 0.3505 mL | 0.8762 mL | |
| 60 mM | 0.0292 mL | 0.1460 mL | 0.2921 mL | 0.7301 mL | |
| 80 mM | 0.0219 mL | 0.1095 mL | 0.2190 mL | 0.5476 mL | |
| 100 mM | 0.0175 mL | 0.0876 mL | 0.1752 mL | 0.4381 mL |
Zefamenib 関連分類
HY-153714 関連分類
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