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Art. -Nr.: HY-183568

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MAT2A-IN-26

MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC₅₀ of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₃H₂₁F₂N₅O₂
Molecular Weight:437.44

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

MAT2A-IN-26 Chemical Structure

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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

MAT2A-IN-26 (Compound 33) (0.01-1 μM; 72 h) potently and selectively inhibits proliferation of HCT116 MTAP KO cells with a GI₅₀ of 0.76 μM, reduces intracellular SAM and sDMA levels in HCT116 MTAP KO cells, and suppresses proliferation of multiple MTAP-null cancer cell lines including MCF-7, H4, and NCI-H838^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-24	Bioavailability	CL	V_ss
Mice^[1]	2 mg/kg	i.v.	5.42 h	0.18 h	9997 ng/mL	88212 ng·h/mL	/	0.37 mL/min/kg	178 mL/kg
Mice^[1]	10 mg/kg	p.o.	10.0 h	1.33 h	35690 ng/mL	426510 ng·h/mL	96.7 %	/	/

In Vivo

MAT2A-IN-26 (Compound 33) (1-10 mg/kg; p.o.; once daily for 14 consecutive days) induces potent, dose-dependent anti-tumor activity in the MTAP-deficient NCI-H838 xenograft mouse model^[1].

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

Animal Model:

SCID mice (female)^[1]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

p.o.; daily
Result:

Exhibited slightly stronger antitumor efficacy than IDE-397 at 1 mg/kg.
Induced tumor regression with mean tumor volumes returning to baseline levels and a tumor growth inhibition (TGI) value of approximately 90% at 10 mg/kg after continuous administration for 8 days.
Caused only a slight decrease in body weight at 10 mg/kg.
Showed dose-dependent reduction in SAM levels in both plasma and tumor tissue, with the most pronounced reduction at 10 mg/kg.
Induced substantial decrease in tumor sDMA levels.

Chemical Information

Molecular Weight 437.44
Formel C₂₃H₂₁F₂N₅O₂
SMILES

CN1C=C2C=C(C=CC2=N1)N3N=CC(NCC4CC4)=C(C3=O)C5=CC=C(C=C5)OC(F)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Zhang Y, et al. Design and Discovery of Pyridazinone-Based MAT2A Inhibitors Targeting MTAP-Deficient Cancers. J Med Chem. 2026;69(9):10104-10121. [Content Brief]

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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