SJF-0628
Based on 1 Customer Validation
SJF-0628 is a PROTAC degrader of BRAF mutants, with a DC50 of 6.8 nM against BRAFV600E. SJF-0628 induces the ubiquitination and degradation of BRAF mutants in various cancer cell lines. SJF-0628 reduces pMEK and pErk levels. SJF-0628 exhibits antitumor activity. SJF-0628 can be used in research on colorectal cancer, melanoma, lung cancer, and triple-negative breast cancer.
(Pink: B-RafV600E ligand (HY-12057); Blue: VHL ligand (HY-125845); Black: linker (HY-W803227)).
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: 99.90%
- CAS 番号: 2413035-41-1
- 分子式: C51H57F2N9O7S2
- 分子量:1010.18
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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MAPK Compound Library
HY-L010
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Anti-Cancer Compound Library
HY-L025
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Oxygen Sensing Compound Library
HY-L045
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Ferroptosis Compound Library
HY-L051
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Colorectal Cancer Compound Library
HY-L103
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Membrane Receptor-targeted Compound Library
HY-L150
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PROTAC Library
HY-L151
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Cell Death Library
HY-L162
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Protein Kinase Compound Library
HY-L196
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
生物活性
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VHL |
BRafV600E 6.8 nM (DC50) |
SJF-0628 (10-1000 nM, 1-48 h) causes concentration-dependent and time-dependent degradation of BRAF V600E and total BRAF and decreases pMEK and pErk levels in DU-4475 cells[1].
SJF-0628 (10-1000 nM, 48 h) results in significant decreases in BRAF levels in Colo-205, LS-411N, HT-29, and RKO colorectal cancer cell lines[1].
SJF-0628 (0.01-1000 nM, 72 h) shows dose-dependent inhibition of cell viability in DU-4475, Colo-205, LS-411N, HT-29, and RKO cells, with IC50 values of 163 nM, 37.6 nM, 96.3 nM, 53.6 nM, and <1 μM respectively, and maximal inhibition of 91.5 %, 85.2 %, 65.2 %, 63.0 %, and 42.0 % respectively[1].
SJF-0628 (1 μM, 72 h) causes time-dependent loss of cell viability in DU-4475 and Colo-205 cells, inducing cleavage of PARP and caspases, indicating apoptosis[1].
SJF-0628 (0.5-1000 nM) dose-dependently degrades relevant BRAF in SK-MEL-239 C4, SK-MEL-246, H1666 and CAL-12-T cells with DC50 of 72, 15, 29, 23 nM, respectively[2].
SJF-0628 (0.001-10 μM, 3-5 days) inhibits cell growth in SK-MEL-28 (EC50 = 37 nM) and reduces growth in SK-MEL-239-C4 (EC50 = 218 nM)[2].
SJF-0628 potently degrades various mutant BRAF proteins (BRAFV600E, BRAF-p61V600E, BRAFG469A, BRAFG466V) in melanoma and lung cancer cell lines, with DC50 values ranging from 6.8 to 72 nM[3].
SJF-0628 potently degrades BRAFV600E with a DC50 of 6.8 nM in SK-MEL-28 cells, without affecting wild-type BRAF[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU-4475 cells
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Concentration:10, 100, 1000 nM
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Incubation Time:1, 24, 48 h
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Result:Caused concentration-dependent and time-dependent degradation of BRAF V600E and total BRAF.
Decreased pMEK and pErk levels.
SJF-0628 (50 mg/kg, i.p., twice daily or 100 mg/kg, i.p., once daily) induces tumor shrinkage beyond initial size in SK-MEL-246 xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A375 cells (5 × 106 in PBS) were subcutaneously implanted into the flanks of female nu/nu mice[2]
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Dosage:50 mg/kg or 150 mg/kg
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Administration:i.p., once daily, 3 days
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Result:Demonstrated marked degradation of BRAF in A375 xenografts with DMAX>90% at doses of 50 mg/kg and 150 mg/kg.
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Animal Model:SK-MEL-246 cells (10 × 106 in PBS) were subcutaneously implanted into the flanks of female nu/nu mice[2]
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Dosage:50 mg/kg or 100 mg/kg
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Administration:i.p. twice daily or i.p. once daily
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Result:Induced tumor shrinkage beyond the initial size in SK-MEL-246 xenografts within 10 days, with 50 mg/kg twice daily showing better efficacy.
Showed no significant body weight loss in mice treated with either 50 mg/kg twice daily or 100 mg/kg once daily.
Reduced MAPK signaling in xenograft tumors, as evidenced by inhibited MEK and ERK phosphorylation.
化学情報
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CAS 番号 2413035-41-1
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性状 Solid
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分子量 1010.18
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分子式 C51H57F2N9O7S2
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Color Off-white to light yellow
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(C4=CN=C(NC=C5C(C6=C(F)C=CC(NS(=O)(CCC)=O)=C6F)=O)C5=C4)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 160 mg/mL (158.39 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 (protect from light). 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 (protect from light). 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: ≥ 4 mg/mL (3.96 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (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
[1]. Chapdelaine AG, et al. The Targeted Degradation of BRAF V600E Reveals the Mechanisms of Resistance to BRAF-Targeted Treatments in Colorectal Cancer Cells. Cancers (Basel). 2023 Dec 12;15(24):5805. [Content Brief]
[2]. Alabi S, et al. Mutant-selective degradation by BRAF-targeting PROTACs. Nat Commun. 2021 Feb 10;12(1):920. [Content Brief]
[3]. He M, et al. Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation. Frontiers in cell and developmental biology. 2021;9:685106. [Content Brief]
[4]. Han X, et al. PROTACs: A novel strategy for cancer drug discovery and development. MedComm. 2023 Jun;4(3):e290. [Content Brief]
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 (protect from light). 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 | 0.9899 mL | 4.9496 mL | 9.8992 mL | 24.7481 mL |
| 5 mM | 0.1980 mL | 0.9899 mL | 1.9798 mL | 4.9496 mL | |
| 10 mM | 0.0990 mL | 0.4950 mL | 0.9899 mL | 2.4748 mL | |
| 15 mM | 0.0660 mL | 0.3300 mL | 0.6599 mL | 1.6499 mL | |
| 20 mM | 0.0495 mL | 0.2475 mL | 0.4950 mL | 1.2374 mL | |
| 25 mM | 0.0396 mL | 0.1980 mL | 0.3960 mL | 0.9899 mL | |
| 30 mM | 0.0330 mL | 0.1650 mL | 0.3300 mL | 0.8249 mL | |
| 40 mM | 0.0247 mL | 0.1237 mL | 0.2475 mL | 0.6187 mL | |
| 50 mM | 0.0198 mL | 0.0990 mL | 0.1980 mL | 0.4950 mL | |
| 60 mM | 0.0165 mL | 0.0825 mL | 0.1650 mL | 0.4125 mL | |
| 80 mM | 0.0124 mL | 0.0619 mL | 0.1237 mL | 0.3094 mL | |
| 100 mM | 0.0099 mL | 0.0495 mL | 0.0990 mL | 0.2475 mL |
SJF-0628 関連分類
HY-136420 関連分類
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