Safimaltib
Based on 2 publication(s) in Google Scholar
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis.
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: 99.63%
- CAS 番号: 2230273-76-2
- 分子式: C20H11F6N5O2
- 分子量:467.32
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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
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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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Immunology/Inflammation Compound Library
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Highly Selective Inhibitors Library
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MedChemExpress（MCE）の使用を引用している文献 Safimaltib
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生物活性
Safimaltib (JNJ-67856633) is effective and highly bioavailable in both mouse and rat tumors, and in some cases led to tumor stasis.
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Safimaltib leads to potent in vivo pharmacodynamic shutdown in CD79b- as well as CARD11-mutant ABC-DLBCL models as measured by serum IL10 or uncleaved BCL10 levels in tumors[1][3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2230273-76-2
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性状 Solid
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分子量 467.32
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分子式 C20H11F6N5O2
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Color Off-white to yellow
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SMILES
O=C(C1=C(C(F)(F)F)N(C2=CC=CC3=C2C=CNC3=O)N=C1)NC4=CC(C(F)(F)F)=NC=C4
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別名
JNJ-67856633
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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
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Cancer
Targeting both death and paracaspase domains of MALT1 with antisense oligonucleotides overcomes resistance to immune-checkpoint inhibitors. [Abstract]2025 Apr;6(4):702-717. PMID: 40075237 -
Autophagy
2024 Dec;20(12):2697-2718. PMID: 39081059
溶剤 & 溶解度
DMSO : 100 mg/mL (213.99 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: ≥ 5 mg/mL (10.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (10.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (278 KB)
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SDS (393 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 | 2.1399 mL | 10.6993 mL | 21.3986 mL | 53.4965 mL |
| 5 mM | 0.4280 mL | 2.1399 mL | 4.2797 mL | 10.6993 mL | |
| 10 mM | 0.2140 mL | 1.0699 mL | 2.1399 mL | 5.3497 mL | |
| 15 mM | 0.1427 mL | 0.7133 mL | 1.4266 mL | 3.5664 mL | |
| 20 mM | 0.1070 mL | 0.5350 mL | 1.0699 mL | 2.6748 mL | |
| 25 mM | 0.0856 mL | 0.4280 mL | 0.8559 mL | 2.1399 mL | |
| 30 mM | 0.0713 mL | 0.3566 mL | 0.7133 mL | 1.7832 mL | |
| 40 mM | 0.0535 mL | 0.2675 mL | 0.5350 mL | 1.3374 mL | |
| 50 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0699 mL | |
| 60 mM | 0.0357 mL | 0.1783 mL | 0.3566 mL | 0.8916 mL | |
| 80 mM | 0.0267 mL | 0.1337 mL | 0.2675 mL | 0.6687 mL | |
| 100 mM | 0.0214 mL | 0.1070 mL | 0.2140 mL | 0.5350 mL |
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