2. PROTAC MAPK/ERK Pathway Apoptosis
  3. Raf PROTACs Apoptosis
  4. SJF-0628

SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912)).

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

SJF-0628

SJF-0628 Chemical Structure

CAS No. : 2413035-41-1

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Customer Review

Based on 1 publication(s) in Google Scholar

SJF-0628 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912))[1].

IC50 & Target[1]

VHL

 

BRafV600E

 

In Vitro

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].

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

SJF-0628 Related Antibodies

Western Blot Analysis[1]

Cell Line: DU-4475 cells
Concentration: 10, 100, 1000 nM
Incubation Time: 1, 24, 48 h
Result: Caused concentration-dependent and time-dependent degradation of BRAF V600E and total BRAF.
Decreased pMEK and pErk levels.
In Vivo

SJF-0628 (50-150 mg/kg, i.p., once daily, 3 days) demonstrates marked BRAF degradation in A375 xenograft model[2].
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.

Animal Model: A375 cells (5 × 106 in PBS) were subcutaneously implanted into the flanks of female nu/nu mice[2]
Dosage: 50 mg/kg or 150 mg/kg
Administration: i.p., once daily, 3 days
Result: Demonstrated marked degradation of BRAF in A375 xenografts with DMAX>90% at doses of 50 mg/kg and 150 mg/kg.
Animal Model: SK-MEL-246 cells (10 × 106 in PBS) were subcutaneously implanted into the flanks of female nu/nu mice[2]
Dosage: 50 mg/kg or 100 mg/kg
Administration: i.p. twice daily or i.p. once daily
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.
Molecular Weight

1010.18

Formula

C51H57F2N9O7S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9899 mL 4.9496 mL 9.8992 mL
5 mM 0.1980 mL 0.9899 mL 1.9798 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 (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.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

V2

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: ≥ 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.
  • Protocol 2

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

    Solubility: ≥ 4 mg/mL (3.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 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 (40.0 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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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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%
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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 (protect from light)

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
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 (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
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
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SJF-0628 Related Classifications

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.

Keywords:

SJF-06282413035-41-1SJF0628SJF 0628RafPROTACsApoptosisRaf kinasesproteolysis targeting chimeraPROTACBRAF V600E mutationcolorectal cancertriple-negative breast cancerintrinsic resistancemitogen-activated protein kinase pathwayInhibitorinhibitorinhibit

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