MS432

Name: MS432
Brand: MedChemExpress
SKU: HY-130602
Rating: 4.5 (1 reviews)

Cat. No.: HY-130602 Purity: 99.78%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

MS432 Chemical Structure

CAS No. : 2672512-44-4

Size	Price	Stock	Quantity
5 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3650	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MS432:

PD0325901-O-C2-dioxolane Get quote

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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

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)

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	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	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.

Molecular Weight

1076.06

Formula

C₅₀H₆₅F₃IN₇O₆S

CAS No.

2672512-44-4

Appearance

Solid

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

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 : 100 mg/mL (92.93 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	0.9293 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

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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 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.
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.
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

mg/kg

Animal weight
(per animal)

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

Purity: 99.78%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (246 KB) HNMR (500 KB) RP-HPLC (256 KB)

Handling Instructions (2659 KB)

References

[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]

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

MS432 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:

MS4322672512-44-4MS 432MS-432PROTACsMEKMitogen-activated protein kinase kinaseMAPKKMAP2KHT29SK-MEL-28COLO 205UACC 257ColoncancerVHLInhibitorinhibitorinhibit

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MS432

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Other Forms of MS432:

MS432 Related Antibodies

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Complete Stock Solution Preparation Table

MS432 Related Classifications

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