Cat. No.: HY-130602

MS432

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MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC₅₀ values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.
(Pink: MEK1 and MEK2 Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker (HY-W014831)).

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Pureté: 99.72%
CAS No.: 2672512-44-4
Formule: C₅₀H₆₅F₃IN₇O₆S
Masse moléculaire:1076.06

Stockage:

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

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

MS432 Chemical Structure

CAS No.: 2672512-44-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC₅₀ values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively^[1]. (Pink: MEK1 and MEK2 Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker (HY-W014831)).

IC₅₀ & Target^[1]

MEK1

31 nM (DC₅₀, in HT29 cells)

MEK2

17 nM (DC₅₀, in HT29 cells)

MEK1

31 nM (DC₅₀, in SK-MEL-28 cells)

MEK2

9.3 nM (DC₅₀, in SK-MEL-28 cells)

Voir tous les produits spécifiques à Isoform PROTACs :

Voir tous les produits spécifiques à Isoform MEK :

Cellular Effect

Cell Line	Type	Value	Description	References
COLO 205	GI₅₀	30 nM Compound: 23; MS432	Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay Antiproliferative activity against human COLO205 cells assessed as reduction in cell growth after 3 days by WST8 assay	[PMID: 31730343]
HT-29	DC₅₀	17 nM Compound: 23; MS432	Protac activity against VHL/MEK2 in human HT-29 cells harboring BRAF V600E variant assessed as degradation of MEK2 after 24 hrs by Western blot analysis Protac activity against VHL/MEK2 in human HT-29 cells harboring BRAF V600E variant assessed as degradation of MEK2 after 24 hrs by Western blot analysis	[PMID: 31730343]
HT-29	DC₅₀	31 nM Compound: 23; MS432	Protac activity against VHL/MEK1 in human HT-29 cells harboring BRAF V600E variant assessed as degradation of MEK1 after 24 hrs by Western blot analysis Protac activity against VHL/MEK1 in human HT-29 cells harboring BRAF V600E variant assessed as degradation of MEK1 after 24 hrs by Western blot analysis	[PMID: 31730343]
HT-29	GI₅₀	130 nM Compound: 23; MS432	Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]
HT-29	GI₅₀	130 μM Compound: 3; MS432	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	DC₅₀	31 nM Compound: 23; MS432	Protac activity against VHL/MEK1 in human SK-MEL-28 cells harboring BRAF V600E variant assessed as degradation of MEK1 after 24 hrs by Western blot analysis Protac activity against VHL/MEK1 in human SK-MEL-28 cells harboring BRAF V600E variant assessed as degradation of MEK1 after 24 hrs by Western blot analysis	[PMID: 31730343]
SK-MEL-28	DC₅₀	9.3 nM Compound: 23; MS432	Protac activity against VHL/MEK2 in human SK-MEL-28 cells harboring BRAF V600E variant assessed as degradation of MEK2 after 24 hrs by Western blot analysis Protac activity against VHL/MEK2 in human SK-MEL-28 cells harboring BRAF V600E variant assessed as degradation of MEK2 after 24 hrs by Western blot analysis	[PMID: 31730343]
SK-MEL-28	GI₅₀	83 nM Compound: 23; MS432	Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human SK-MEL-28 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]
SK-MEL-28	GI₅₀	83 nM Compound: 3; MS432	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]
UACC-257	GI₅₀	30 nM Compound: 23; MS432	Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay Antiproliferative activity against human UACC257 cells assessed as reduction in cell growth after 3 days by MTT assay	[PMID: 31730343]

In Vitro

MS432 (compound 23) is potent in reducing MEK1/2 protein levels in COLO 205 cells (DC₅₀ (MEK1) = 18 ± 7 nM, DC₅₀ (MEK2) = 11 ± 2 nM) and UACC257 cells (DC₅₀ (MEK1) = 56 ± 25 nM, DC₅₀ (MEK2) = 27 ± 19 nM).

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

Cell Viability Assay^[1]

Cell Line:

(HT-29, SK-MEL-28, COLO 205 and UACC 257 cell lines.
Concentration:

0-1 μM.
Incubation Time:

72 hours.
Result:

Effectively inhibited proliferation of these CRC and melanoma cells in a concentration-dependent manner, with GI₅₀ values ranging from 30 to 200 nM.

In Vivo

MS432 (compound 23) displays good plasma exposure, which is approximately 3 to 20-fold higher than the GI₅₀ values of compound 23 in the tested cancer cell lines^[1].

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

Animal Model:

Male Swiss Albino mice^[1].
Dosage:

50 mg/kg (Pharmacokinetic Analysis).
Administration:

IP
Result:

Displays good plasma exposure with the maximum plasma concentration of 1,400 nM detected at 0.5 hour post dosing and plasma concentration of 710 nM at 8 hours post dosing.

Chemical Information

CAS No. 2672512-44-4
Appearance Solid
Masse moléculaire 1076.06
Formule C₅₀H₆₅F₃IN₇O₆S
Color White to off-white
SMILES

O=C([C@H]1N(C([C@H](C(C)(C)C)NC(CCCCCCCCCCNCCCONC(C2=CC=C(F)C(F)=C2NC3=CC=C(I)C=C3F)=O)=O)=O)C[C@H](O)C1)N[C@H](C4=CC=C(C5=C(C)N=CS5)C=C4)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (92.93 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

0.9293 mL

4.6466 mL

9.2932 mL

5 mM

0.1859 mL

0.9293 mL

1.8586 mL

10 mM

0.0929 mL

0.4647 mL

0.9293 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 (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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.32 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 2

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

Solubility: ≥ 2.5 mg/mL (2.32 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[1]. Wei J, et al. Discovery of a First-in-Class Mitogen-Activated Protein Kinase Kinase 1/2 Degrader. J Med Chem. 2019 Dec 12;62(23):10897-10911. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.9293 mL	4.6466 mL	9.2932 mL	23.2329 mL
	5 mM	0.1859 mL	0.9293 mL	1.8586 mL	4.6466 mL
	10 mM	0.0929 mL	0.4647 mL	0.9293 mL	2.3233 mL
	15 mM	0.0620 mL	0.3098 mL	0.6195 mL	1.5489 mL
	20 mM	0.0465 mL	0.2323 mL	0.4647 mL	1.1616 mL
	25 mM	0.0372 mL	0.1859 mL	0.3717 mL	0.9293 mL
	30 mM	0.0310 mL	0.1549 mL	0.3098 mL	0.7744 mL
	40 mM	0.0232 mL	0.1162 mL	0.2323 mL	0.5808 mL
	50 mM	0.0186 mL	0.0929 mL	0.1859 mL	0.4647 mL
	60 mM	0.0155 mL	0.0774 mL	0.1549 mL	0.3872 mL
	80 mM	0.0116 mL	0.0581 mL	0.1162 mL	0.2904 mL

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MS432

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform MEK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MS432

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Angiogenesis-Related Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

PROTAC Library

Multi-Target Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Voir tous les produits spécifiques à Isoform PROTACs

Voir tous les produits spécifiques à Isoform MEK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

MS432 Related Classifications

HY-130602 Related Classifications