2. PROTAC Metabolic Enzyme/Protease Apoptosis
  3. PROTACs Tyrosinase Apoptosis
  4. MS105

MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research.
(Pink: BRK Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W105727)).

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

MS105

MS105 Chemical Structure

CAS No. : 2408339-39-7

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Based on 1 publication(s) in Google Scholar

MS105 Related Antibodies

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View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) (BRK) PROTAC degrader. MS105 recruits VHL E3 ligase via a VHL ligand moiety, promotes PTK6 ubiquitination and proteasomal degradation, inhibits the proliferation and migration of breast cancer cells, and induces apoptosis. MS105 shows potential for use in breast cancer research[1]. (Pink: BRK Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker (HY-W105727)).

In Vitro

MS105 binds to PTK6 with a Kd of 730 nM in a cell-free competitive displacement assay[1].
MS105 (1 μM) inhibits the in vitro activity of PTK6 and 5 additional kinases by >65% in a cell-free KINOMEScan assay[1].
MS105 (0.07-1.25 μM; 24 h) potently reduces PTK6 protein levels in T47D human ER+ breast cancer cells[1].
MS105 (0.003-1.25 μM; 4-72 h) potently degrades PTK6 in MDA-MB-231/LM2-4 human triple negative breast cancer cells with a DC50 of 21 nM and Dmax of 84%, with detectable degradation as early as 8 hours and persistence for up to 72 hours[1].
MS105 (0.07-0.3 μM) degrades PTK6 in MDA-MB-231/LM2-4 human triple negative breast cancer cells via a proteasome- and VHL-dependent mechanism, as pre-treatment with proteasome, VHL, or NEDD8-activating enzyme inhibitors abrogates PTK6 degradation[1].
MS105 (0.16-0.3 μM) requires direct binding to PTK6 to induce degradation in MDA-MB-231/LM2-4 human triple negative breast cancer cells, as pre-treatment with the high-affinity PTK6 inhibitor P21d blocks PTK6 degradation[1].
MS105 (dose range; 72 h) potently inhibits viability of multiple human breast cancer cell lines (triple negative, ER+, Her2+), with EC50 values ranging from 0.47 to 0.93 μM[1].
MS105 (1 μM; up to 12 days) degrades PTK6 but does not inhibit cell viability or growth in MCF10A human non-transformed mammary epithelial cells or CAPAN-2 human pancreatic cancer cells[1].
MS105 (0.3-1 μM; 24 h) induces apoptosis of MDA-MB-231/LM2-4 human triple negative breast cancer cells and T47D human ER+ breast cancer cells, as evidenced by increased caspase 3/7 activity, cleaved PARP, Bim upregulation, and p38 activation[1].
MS105 (0.6-1 μM; 24 h pre-treatment + 12 h migration) potently inhibits migration of MDA-MB-231 human triple negative breast cancer cells[1].

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

MS105 Related Antibodies

Western Blot Analysis[1]

Cell Line: T47D human ER+ breast cancer cells
Concentration: 0.07-1.25 μM
Incubation Time: 24 h
Result: Reduced PTK6 protein levels across all tested concentrations, with more significant reduction observed at lower concentrations consistent with a PROTAC "hook effect".

Western Blot Analysis[1]

Cell Line: MDA-MB-231/LM2-4 human triple negative breast cancer cells
Concentration: 0.003-1.25 μM (24 h degradation assay); 0.3-1 μM (time-course 4-24 h); 0.3-0.6 μM (time-course 24-72 h)
Incubation Time: 24 h (DC50/Dmax assay); 4-72 h (time-course assay)
Result: Reduced PTK6 protein levels with a DC50 (50% maximum degradation) of 21 nM and a Dmax (maximum degradation) of 84% after 24-hour treatment.
Detected PTK6 degradation as early as 8 hours post-treatment, and downregulation persisted for up to 72 hours.

Cell Viability Assay[1]

Cell Line: Multiple human breast cancer cell lines: MDA-MB-231, HCC1806, MDA-MB-231/LM2-4, T47D, MCF7, MDA-MB-453
Concentration: dose range
Incubation Time: 72 h
Result: Inhibited cell viability with EC50 values of 0.75 μM (MDA-MB-231), 0.93 μM (HCC1806), 0.47 μM (MDA-MB-231/LM2-4), 0.67 μM (T47D), 0.7 μM (MCF7), and 0.52 μM (MDA-MB-453).

Cell Viability Assay[1]

Cell Line: MCF10A human non-transformed mammary epithelial cells, CAPAN-2 human pancreatic cancer cells
Concentration: 1 μM (viability/growth assay); 0.3-2.5 μM (PTK6 degradation assessment)
Incubation Time: up to 10 days (MCF10A viability/growth); up to 12 days (CAPAN-2 viability/growth)
Result: Degraded PTK6 in both cell lines but did not inhibit cell viability or growth in either cell line.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231/LM2-4 and T47D human breast cancer cells
Concentration: 0.3-1 μM
Incubation Time: 24 h
Result: Significantly increased caspase 3/7 activity, induced cleavage of PARP, upregulated all isoforms of Bim protein expression (Bim_EL, Bim_L, Bim_S), and activated p38 phosphorylation in both cell lines.

Cell Migration Assay[1]

Cell Line: MDA-MB-231 human triple negative breast cancer cells
Concentration: 0.6-1 μM
Incubation Time: 24 h (pre-treatment); 12 h (transwell migration assay)
Result: Significantly reduced the number of migrated cells at both tested concentrations.
In Vivo

MS105 (50 mg/kg; i.p.; single dose) administered via intraperitoneal injection in male Swiss Albino mice yields measurable plasma concentrations over a 24-hour period[1].

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

Animal Model: Swiss Albino (male)[1]
Dosage: 50 mg/kg
Administration: i.p.; single dose
Result: Reached measurable plasma concentrations at 0.5, 2, 4, 8, 12 and 24 hours post-administration.
Molecular Weight

1072.30

Formula

C56H70FN13O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@@H](NC(CCCCCCCCNC(CN2CCN(C(C3=CC=C(NC4=NC(C5CC5)=CN6C4=NC=C6C7=CNN=C7)C(F)=C3)=O)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC8=CC=C(C9=C(C)N=CS9)C=C8
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (93.26 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 0.9326 mL 4.6629 mL 9.3257 mL
5 mM 0.1865 mL 0.9326 mL 1.8651 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. 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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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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: ≥ 2.5 mg/mL (2.33 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.33 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 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.
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:
%
DMSO +
% 
+
%
Tween-80 +
%
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).
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. 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 0.9326 mL 4.6629 mL 9.3257 mL 23.3144 mL
5 mM 0.1865 mL 0.9326 mL 1.8651 mL 4.6629 mL
10 mM 0.0933 mL 0.4663 mL 0.9326 mL 2.3314 mL
15 mM 0.0622 mL 0.3109 mL 0.6217 mL 1.5543 mL
20 mM 0.0466 mL 0.2331 mL 0.4663 mL 1.1657 mL
25 mM 0.0373 mL 0.1865 mL 0.3730 mL 0.9326 mL
30 mM 0.0311 mL 0.1554 mL 0.3109 mL 0.7771 mL
40 mM 0.0233 mL 0.1166 mL 0.2331 mL 0.5829 mL
50 mM 0.0187 mL 0.0933 mL 0.1865 mL 0.4663 mL
60 mM 0.0155 mL 0.0777 mL 0.1554 mL 0.3886 mL
80 mM 0.0117 mL 0.0583 mL 0.1166 mL 0.2914 mL
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MS105 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:

MS1052408339-39-7YX39-105MS 105MS-105PROTACsTyrosinaseApoptosisBimER+ breast cancer cellsbreast cancer cellsVHLtriple negative breast cancer cellsapoptosisPTK6p38proteasomeHer2+ breast cancer cellsInhibitorinhibitorinhibit

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