1. PROTAC MAPK/ERK Pathway
  2. PROTACs Raf
  3. PROTAC B-Raf degrader 1

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

For research use only. We do not sell to patients.

PROTAC B-Raf degrader 1 Chemical Structure

PROTAC B-Raf degrader 1 Chemical Structure

CAS No. : 2364367-27-9

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Based on 1 publication(s) in Google Scholar

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Description

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity[1].

IC50 & Target[1]

B-Raf

 

In Vitro

The IC50 values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively[1].
? PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].
? MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM[1].
? PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells.
Concentration: 0-200 μM.
Incubation Time: 72 hours.
Result: The IC50 values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively.

Western Blot Analysis[1]

Cell Line: Human MCF-7 breast cancer cell line.
Concentration: 5 or 10 μM.
Incubation Time: 24 hours.
Result: Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1.

Apoptosis Analysis[1]

Cell Line: Human MCF-7 breast cancer cell line.
Concentration: 2.7-20 μM.
Incubation Time: 24 hours.
Result: Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM.

Cell Cycle Analysis[1]

Cell Line: Human MCF-7 breast cancer cell line.
Concentration: 20 μM.
Incubation Time: 24 hours.
Result: 1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase.
Molecular Weight

763.77

Formula

C36H37N5O12S

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CNC(CNC4=CC(CS(=O)(/C=C/C5=C(OC)C=C(OC)C=C5OC)=O)=CC=C4OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (32.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3093 mL 6.5465 mL 13.0929 mL
5 mM 0.2619 mL 1.3093 mL 2.6186 mL
View the 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.27 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.27 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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 (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.78%

References

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 (stored under nitrogen). 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 1.3093 mL 6.5465 mL 13.0929 mL 32.7324 mL
5 mM 0.2619 mL 1.3093 mL 2.6186 mL 6.5465 mL
10 mM 0.1309 mL 0.6546 mL 1.3093 mL 3.2732 mL
15 mM 0.0873 mL 0.4364 mL 0.8729 mL 2.1822 mL
20 mM 0.0655 mL 0.3273 mL 0.6546 mL 1.6366 mL
25 mM 0.0524 mL 0.2619 mL 0.5237 mL 1.3093 mL
30 mM 0.0436 mL 0.2182 mL 0.4364 mL 1.0911 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PROTAC B-Raf degrader 1
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