Art. -Nr.: HY-132301

MSC-4381

Name: MSC-4381
Brand: MedChemExpress
SKU: HY-132301
Price: 190.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: MCT4-IN-1)

Kundenbewertung

Based on 1 Customer Validation

MSC-4381 (MCT4-IN-1), a chemical probe, is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC₅₀ of 77 nM and a K_i of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 98.89%
CAS. Nr.: 2445185-57-7
Formel: C₂₆H₂₀ClN₃O₆S
Molecular Weight:537.97

Speicherung:

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

MSC-4381 Chemical Structure

CAS. Nr.: 2445185-57-7

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (3)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MSC-4381 (MCT4-IN-1), a chemical probe, is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC₅₀ of 77 nM and a K_i of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research^[1]. MSC-4381 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

MCT4

77 nM (IC₅₀)

MCT4

11 nM (Ki)

Alle Monocarboxylate Transporter Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC₅₀	1 nM Compound: 18n	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis Cytotoxicity against human MDA-MB-231 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis	[PMID: 34382802]
MDA-MB-231	IC₅₀	11 nM Compound: 18n	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay	[PMID: 34382802]
MIA PaCa-2	IC₅₀	4720 nM Compound: 18n	Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay Cytotoxicity against human MIA PaCa-2 cells assessed as inhibition of cell growth incubated for 6 days by MTS assay	[PMID: 34382802]
MIA PaCa-2	IC₅₀	>25000 nM Compound: 18n	Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis Cytotoxicity against human MIA PaCa-2 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis	[PMID: 34382802]
NCI-H358	IC₅₀	3 nM Compound: 18n	Cytotoxicity against human NCI-H358 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis Cytotoxicity against human NCI-H358 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis	[PMID: 34382802]
RT-4	IC₅₀	638 nM Compound: 18n	Cytotoxicity against human RT-4 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis Cytotoxicity against human RT-4 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis	[PMID: 34382802]
SNU-398	IC₅₀	>25000 nM Compound: 18n	Cytotoxicity against human SNU-398 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis Cytotoxicity against human SNU-398 cells assessed as reduction in intracellular lactate accumulation preincubated for 30 mins followed by D(+)glucose and measured after 4 hrs by UHPLC-ESI-Q-Orbitrap-MS analysis	[PMID: 34382802]

In Vitro

MSC-4381 (compound 18n) inhibits lactate efflux in the MDA-MB-231 cell line with an IC₅₀ of 1 nM. The on-target activity is confirmed with a K_i of 11 nM by fluorescence cross-correlation spectroscopy (FCCS)^[1].
MSC-4381 does not inhibit lactate efflux to a similar extent in SNU-398 and MiaPaca2, and only 600-fold less in RT-4 cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

MSC-4381 (compound 18n; 30 mg/kg; PO; single dose) only combined with MCT1/2 inhibitor exhibits a significant tumoral intracellular lactate accumulation^[1].
MSC-4381 (30 mg/kg/day; for 15 days) shows no significant antitumor activity^[1].
MSC-4381 (0.2 mg/kg; iv) has a T_1/2 of 1 hours, a CL of 0.33 L/h kg, a C_max of 489 ng/mL and a V_ss of 0.4 L/kg for mice^[1].

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

Animal Model:

MC38 tumor-bearing C57/BL6 mice^[1]
Dosage:

30 mg/kg
Administration:

PO; single dose
Result:

Only combined with MCT1/2 inhibitor exhibited a significant tumoral intracellular lactate accumulation.

Animal Model:

Mice^[1]
Dosage:

0.2 mg/kg (Pharmacokinetic Analysis)
Administration:

IV
Result:

Had a T_1/2 of 1 hours, a CL of 0.33 L/h•kg, a C_max of 489 ng/mL and a V_ss of 0.4 L/kg for mice.

Chemical Information

CAS. Nr. 2445185-57-7
Appearance Solid
Molecular Weight 537.97
Formel C₂₆H₂₀ClN₃O₆S
Color White to yellow
SMILES

O=C(C1=NC=C(C#CC2=CC(Cl)=CC=C2NS(=O)(C3=C4N=CC=CC4=C(OCC)C=C3)=O)C(OC)=C1)O
Synonyms

MCT4-IN-1
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 : 83.33 mg/mL (154.90 mM; ultrasonic and warming and heat to 60°C; 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

1.8588 mL

9.2942 mL

18.5884 mL

5 mM

0.3718 mL

1.8588 mL

3.7177 mL

10 mM

0.1859 mL

0.9294 mL

1.8588 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: ≥ 2.08 mg/mL (3.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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

Protokoll

All Cell Biology

EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)
Handling Instructions (2659 KB)

Verweise

[1]. Timo Heinrich, et al. Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology. J Med Chem. 2021 Aug 26;64(16):11904-11933. [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	1.8588 mL	9.2942 mL	18.5884 mL	46.4710 mL
	5 mM	0.3718 mL	1.8588 mL	3.7177 mL	9.2942 mL
	10 mM	0.1859 mL	0.9294 mL	1.8588 mL	4.6471 mL
	15 mM	0.1239 mL	0.6196 mL	1.2392 mL	3.0981 mL
	20 mM	0.0929 mL	0.4647 mL	0.9294 mL	2.3235 mL
	25 mM	0.0744 mL	0.3718 mL	0.7435 mL	1.8588 mL
	30 mM	0.0620 mL	0.3098 mL	0.6196 mL	1.5490 mL
	40 mM	0.0465 mL	0.2324 mL	0.4647 mL	1.1618 mL
	50 mM	0.0372 mL	0.1859 mL	0.3718 mL	0.9294 mL
	60 mM	0.0310 mL	0.1549 mL	0.3098 mL	0.7745 mL
	80 mM	0.0232 mL	0.1162 mL	0.2324 mL	0.5809 mL
	100 mM	0.0186 mL	0.0929 mL	0.1859 mL	0.4647 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

MSC-4381

Alle Monocarboxylate Transporter Isoform-spezifische Produkte anzeigen