2. PROTAC MAPK/ERK Pathway
  3. PROTACs MEK
  4. MS934

MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma.
(Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078))

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

MS934 Chemical Structure

MS934 Chemical Structure

CAS No. : 2756323-15-4

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1 mg USD 400 In-stock
5 mg USD 1200 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

MS934 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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MEK1 MEK2 MEK5 MEK

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 has anti-proliferation potency at inhibiting the growth of HT-29 cells with a GI50 value of 0.023 μM. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma[1].
(Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078))

IC50 & Target

GI50: 0.023 μM (HT-29 cells)[1]
Cellular Effect
Cell Line Type Value Description References
HT-29 GI50
23 μM
Compound: 27; MS934
Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human HT-29 cells incubated for 3 days by WST8 assay
[PMID: 33284613]
SK-MEL-28 GI50
40 nM
Compound: 27; MS934
Antiproliferative activity against human SK-MEL-28 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SK-MEL-28 cells incubated for 3 days by WST8 assay
[PMID: 33284613]
SU-DHL-1 GI50
330 nM
Compound: 27; MS934
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
Antiproliferative activity against human SU-DHL-1 cells incubated for 3 days by WST8 assay
[PMID: 33284613]
Molecular Weight

1104.11

Formula

C52H69F3IN7O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(C(F)=C(C=C1)F)NC2=C(C=C(C=C2)I)F)NOCCCCNCCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N3[C@@H](C[C@H](C3)O)C(N[C@H](C4=CC=C(C5=C(N=CS5)C)C=C4)C)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (45.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9057 mL 4.5285 mL 9.0571 mL
5 mM 0.1811 mL 0.9057 mL 1.8114 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 1.25 mg/mL (1.13 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.
  • Protocol 2

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

    Solubility: ≥ 1.25 mg/mL (1.13 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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 +
% 
+
%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, 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
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, 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 0.9057 mL 4.5285 mL 9.0571 mL 22.6427 mL
5 mM 0.1811 mL 0.9057 mL 1.8114 mL 4.5285 mL
10 mM 0.0906 mL 0.4529 mL 0.9057 mL 2.2643 mL
15 mM 0.0604 mL 0.3019 mL 0.6038 mL 1.5095 mL
20 mM 0.0453 mL 0.2264 mL 0.4529 mL 1.1321 mL
25 mM 0.0362 mL 0.1811 mL 0.3623 mL 0.9057 mL
30 mM 0.0302 mL 0.1510 mL 0.3019 mL 0.7548 mL
40 mM 0.0226 mL 0.1132 mL 0.2264 mL 0.5661 mL
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MS934 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:

MS9342756323-15-4MS 934MS-934PROTACsMEKMitogen-activated protein kinase kinaseMAPKKMAP2KVHL-recruitingMEK 1/2HT-29 cellscancersmelanomanonsmall cell lung cancer (NSCLC)colorectal cancerprimary brain tumorshepatocellular carcinomaInhibitorinhibitorinhibit

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