Aminopterin

Catalog No.E1003 Batch:E100301

Technical Data

Formula	C₁₉H₂₀N₈O₅
Molecular Weight	440.41	CAS No.	54-62-6
Solubility (25°C)*	In vitro	DMSO	88 mg/mL (199.81 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Aminopterin (4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739), a folic acid antagonist, is a competitive inhibitor of dihydrofolate reductase (DHFR) with Ki of 3.7 pM.

Targets

folic acid ^[1]	DHFR ^[2] (Cell-free assay)
	3.7 pM(Ki)

In vitro

In lymphoma celllines and several acute lymphoblastic leukaemia (ALL) cell lines (including COG-LL-356, NALM-6 and CCRF-CEM), the intensity of the cell kill effect, defined as maximal inhibition at the concentrations tested, is greater with Aminopterin than Methotrexate.^[3]

In vivo

In NOD/SCID mice, Aminopterin significantly delays the progression of ALL-3, ALL-16 and ALL-19, but not ALL-8 xenografts.^[3]

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines lymphoma celllines and several ALL cell lines (including COG-LL-356, NALM-6 and CCRF-CEM) Concentrations 1 nM - 10 μM Incubation Time 72 h Method The concentrations of Aminopterin tested are 1 × 10^-9 to 1 × 10^-5 mol/l in threefold changes (1 × 10^-9, 3 × 10^-9, 1 × 10^-8, 3 × 10^-8, 1 × 10^-7, 3 × 10^-7, 1 × 10^-6, 3 × 10^-6, 1 × 10^-5 mol/l). Cells are incubated with vehicle control or drugs for 72 h.
Animal Study:^{^[3]}	Animal Models NOD/SCID mice Dosages 0.5 mg/kg, 0.25 mg/kg Administration i.p.

Cell Assay:^{^[3]}

Cell lines
lymphoma celllines and several ALL cell lines (including COG-LL-356, NALM-6 and CCRF-CEM)
Concentrations
1 nM - 10 μM
Incubation Time
72 h
Method
The concentrations of Aminopterin tested are 1 × 10^-9 to 1 × 10^-5 mol/l in threefold changes (1 × 10^-9, 3 × 10^-9, 1 × 10^-8, 3 × 10^-8, 1 × 10^-7, 3 × 10^-7, 1 × 10^-6, 3 × 10^-6, 1 × 10^-5 mol/l). Cells are incubated with vehicle control or drugs for 72 h.

Animal Study:^{^[3]}

Animal Models
NOD/SCID mice
Dosages
0.5 mg/kg, 0.25 mg/kg
Administration
i.p.

References

Selleck's Aminopterin has been cited by 1 publication

Metabolic Hallmarks for Purine Nucleotide Biosynthesis in Small Cell Lung Carcinoma [ Mol Cancer Res, 2024, 22(1):82-93]	PubMed: 37773022

Metabolic Hallmarks for Purine Nucleotide Biosynthesis in Small Cell Lung Carcinoma [ Mol Cancer Res, 2024, 22(1):82-93]

PubMed: 37773022

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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