Belvarafenib
Based on 6 publication(s) in Google Scholar
Belvarafenib (HM95573) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF 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。
- 純度: 98.97%
- CAS 番号: 1446113-23-0
- 分子式: C23H16ClFN6OS
- 分子量:478.93
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
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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生物活性
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BRafV600E 7 nM (IC50) |
CRAF 5 nM (IC50) |
B-Raf 56 nM (IC50) |
Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively[1].
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 1446113-23-0
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性状 Solid
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分子量 478.93
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分子式 C23H16ClFN6OS
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Color Off-white to yellow
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SMILES
O=C(C(C1=NC=N2)=CSC1=C2N)NC(C3=C4C(NC(C=CC=C5Cl)=C5F)=NC=C3)=C(C=C4)C
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別名
HM95573; GDC-5573; RG6185
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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, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
mTOR inhibition enhances the antitumor efficacy of pan-RAF-MEK blockade by inhibiting the ATF4-MTHFD2 pathway. [Abstract]2026 May 6;17(1):600. PMID: 42091854
Belvarafenib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
Fold change of MTHFD2 transcripts following indicated treatment in WM3406 cells (left) and MeWo cells (right) treated with INK128, Cobimetinib and Belvarafenib (25 nM).
Belvarafenib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
Western blot analysis of the indicated proteins in WM3406 (left) and MeWo (right) cells with ATF4 knockdown or Belvarafenib (25 nM) plus Cobimetinib treatment.
Belvarafenib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
Percent apoptosis detected in DMSO- or Belvarafenib plus Cobimetinib- or Belvarafenib (25 nM) plus Cobimetinib plus nucleosides-treated WM3406 or MeWo cells.
Belvarafenib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
Representative images of WM3406 and MeWo cells following Belvarafenib plus Cobimetinib- or Belvarafenib (25 nM) plus Cobimetinib plus nucleosides-treated for 18 h and processed for γH2AX (green) immunofluorescence.
Belvarafenib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2026 May 6;17(1):600. [Abstract]
Tumor growth curve comparing MaNRAS1007 melanomas grown on C57BL/6N host mice with or without Belvarafenib (5 mg/kg, i.g.) plus Cobimetinib treatments.
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Proc Natl Acad Sci U S A
2023 Oct 10;120(41):e2308635120. PMID: 37782788 -
J Invest Dermatol
Combined Inhibition of MNK Signaling and BET Proteins Reveals TGM2 as a Novel Vulnerability in Melanoma. [Abstract]2025 Apr;145(4):979-984.e5. PMID: 39357785 -
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溶剤 & 溶解度
DMSO : 12.5 mg/mL (26.10 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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: ≥ 1.25 mg/mL (2.61 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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, 1 year; -20°C, 6 months (stored under nitrogen)
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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取扱説明書 (2659 KB)
参考文献
[1]. WO 2013/100632 A1.
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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0880 mL | 10.4399 mL | 20.8799 mL | 52.1997 mL |
| 5 mM | 0.4176 mL | 2.0880 mL | 4.1760 mL | 10.4399 mL | |
| 10 mM | 0.2088 mL | 1.0440 mL | 2.0880 mL | 5.2200 mL | |
| 15 mM | 0.1392 mL | 0.6960 mL | 1.3920 mL | 3.4800 mL | |
| 20 mM | 0.1044 mL | 0.5220 mL | 1.0440 mL | 2.6100 mL | |
| 25 mM | 0.0835 mL | 0.4176 mL | 0.8352 mL | 2.0880 mL |
Belvarafenib 関連分類
HY-109080 関連分類
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