Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie
 
> 7ACC2 [1472624-85-3]

7ACC2 [1472624-85-3]

Drucken Drucken
Melden Sie sich an

Katalog-Nummer HY-D0713-5mg

Size : 5mg

Marke : MedChemExpress

Weitere Informationen anfordern

Contact local distributor :


Telefonnummer : +1 850 650 7790

Beschreibung

7ACC2 is a potent monocarboxylate transporter (MCT) inhibitor with an IC50 of 11 nM for inhibition of [14C]-lactate influx. 7ACC2 is also a potent inhibitor of mitochondrial pyruvate transport. 7ACC2 is an anticancer agent through inhibition of lactate flux[1][2].

IC50 & Target

IC50: 11 nM (Monocarboxylate transporter)[1]
Mitochondrial pyruvate transport[2]
Cellular Effect
Cell Line Type Value Description References
SiHa IC50
0.059 μM
Compound: 19
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 24 hrs by liquid scintillation counting
[PMID: 24095010]
SiHa EC50
0.22 μM
Compound: 19
Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
Cytotoxicity against human SiHa cells in lactate-containing medium after 72 hrs by MTT assay
[PMID: 24095010]
SiHa IC50
10 nM
Compound: 19
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
Inhibition of MCT4-mediated [14C]-lactate uptake in human SiHa cells in lactate-containing medium assessed as remaining lactate concentration in culture medium after 12 mins by liquid scintillation counting
[PMID: 24095010]
In Vitro

7ACC2 (compound 19; 72 hours) inhibits SiHa cells proliferation in lactate-containing medium with an EC50 of 0.22 μM. In SiHa cells, lactate uptake primarily depends on the high affinity MCT1 transporter[1].
7ACC2 (compound 19) shows an excellent chemical stability in simulated gastric (SGF) and intestinal (SIF) fluids, a good apparent permeability coefficient (Papp) through Caco-2 monolayer and a high metabolic stability on mouse (MLM) and human liver microsomes (HLM) as well as on human hepatocytes[1].
7ACC2 is a potent inhibitor of mitochondrial pyruvate transport which consecutively blocks extracellular lactate uptake by promoting intracellular pyruvate accumulation[2].

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

7ACC2 Related Antibodies
In Vivo

7ACC2 (3?mg/kg; intraperitoneal administration; daily; for 5 days or 10days) treatment significantly inhibits tumor growth in mice. 7ACC2 radiosensitizes tumor cells by reducing hypoxia in vivo[2].
The intraperitoneal administration of 7ACC2 (compound 19; 3 mg/kg) to mice leads to a Cmax of 1246 ng/ml (4 μM) in a very short time (Tmax=10 min) associated with a plasma half-life of 4.5 h[1].

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

Animal Model: 7-week-old female NMRI nude mice with radiotherapy administered[2]
Dosage: 3 mg/kg
Administration: Intraperitoneal administration; daily; for 5 days or 10days
Result: A significant increase in tumor growth delay was observed.
Molekulargewicht

309.32

Formel

C18H15NO4
CAS. Nr.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CN(C1=CC=C(C=C(C(O)=O)C(O2)=O)C2=C1)CC3=CC=CC=C3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 50 mg/mL (161.64 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 3.2329 mL 16.1645 mL 32.3290 mL
5 mM 0.6466 mL 3.2329 mL 6.4658 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: 2.5 mg/mL (8.08 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Reinheit & Dokumentation
Verweise

Sie könnten auch an folgenden Produkten interessiert sein:



Katalog-Nummer
Beschreibung
Cond.
Preis zzgl. MwSt.
HY-112812-5mg
SCD1 inhibitor-1 [1069094-65-0]
 5mg 
KA1674
Pyruvate Assay Kit
 1Kit