Art. -Nr.: HY-171830

MS105

(Synonyms: YX39-105)

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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)).

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Reinheit: 98.27%
CAS. Nr.: 2408339-39-7
Formel: C₅₆H₇₀FN₁₃O₆S
Molecular Weight:1072.30

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS105 Chemical Structure

CAS. Nr.: 2408339-39-7

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)).

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

MS105 binds to PTK6 with a K_d 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.

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.

Chemical Information

CAS. Nr. 2408339-39-7
Appearance Solid
Molecular Weight 1072.30
Formel C₅₆H₇₀FN₁₃O₆S
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
Synonyms

YX39-105
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9326 mL

4.6629 mL

9.3257 mL

5 mM

0.1865 mL

0.9326 mL

1.8651 mL

10 mM

0.0933 mL

0.4663 mL

0.9326 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (2.33 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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Martinez C, et al. A PROTAC degrader suppresses oncogenic functions of PTK6, inducing apoptosis of breast cancer cells. Cell Chem Biol. 2025;32(2):255-266.e8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Alle PROTACs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS105 Related Classifications

HY-171830 Related Classifications