TBAP-001
Based on 1 Customer Validation
TBAP-001 (Synthesis 13), extracted from patent WO2015075483A1, is a pan-RAF kinase inhibitor, with an IC50 of 62 nM in BRAF V600E kinase assay.
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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。
- 純度: 98.97%
- CAS 番号: 1777832-90-2
- 分子式: C27H23F2N7O3
- 分子量:531.51
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
生物活性
IC50: 62 nM (BRAF V600E kinase assay), 18 nM (Cell-Based Phosho-ERK Assay)[1].
BAP-001 (Synthesis 13) exhibits IC50 values of 178 nM (A375), 62 nM (WM266.4), 72 nM (UACC62), 93 nM (LOX INVI), 590 nM (HT 29), 43 nM (COLO225), 690 nM (RKO), 490 nM (Mawi), 390 nM (WiDr), 480 nM (Colo741), 480 nM (SW620), 600 nM (HCT116), 390 nM (SKMEL2), 710 nM (D04), 390 nM (WM1361), 1150 nM (PDAC R172H (p53 mut)), 290 nM (MiaPaCa) and 490nM (RPMI8226) in different cancer cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1777832-90-2
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性状 Solid
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分子量 531.51
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分子式 C27H23F2N7O3
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Color Off-white to yellow
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SMILES
O=C(NC1=CC(C(C)(C)C)=NN1C2=CC=CC(F)=C2)NC3=CC=C(OC4=C(N=C5)C(NC5=O)=NC=C4)C=C3F
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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 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 250 mg/mL (470.36 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: 2.08 mg/mL (3.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (274 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8814 mL | 9.4072 mL | 18.8143 mL | 47.0358 mL |
| 5 mM | 0.3763 mL | 1.8814 mL | 3.7629 mL | 9.4072 mL | |
| 10 mM | 0.1881 mL | 0.9407 mL | 1.8814 mL | 4.7036 mL | |
| 15 mM | 0.1254 mL | 0.6271 mL | 1.2543 mL | 3.1357 mL | |
| 20 mM | 0.0941 mL | 0.4704 mL | 0.9407 mL | 2.3518 mL | |
| 25 mM | 0.0753 mL | 0.3763 mL | 0.7526 mL | 1.8814 mL | |
| 30 mM | 0.0627 mL | 0.3136 mL | 0.6271 mL | 1.5679 mL | |
| 40 mM | 0.0470 mL | 0.2352 mL | 0.4704 mL | 1.1759 mL | |
| 50 mM | 0.0376 mL | 0.1881 mL | 0.3763 mL | 0.9407 mL | |
| 60 mM | 0.0314 mL | 0.1568 mL | 0.3136 mL | 0.7839 mL | |
| 80 mM | 0.0235 mL | 0.1176 mL | 0.2352 mL | 0.5879 mL | |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.4704 mL |