Home Metabolism DHFR inhibitor Aminopterin For research use only.

Aminopterin

Synonyms: 4-amino Folic Acid, 4-amino PGA, 4-Aminofolic acid, 4-Aminopteroylglutamic acid, Aminopteroylglutamic acid, APGA, NSC 739

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.

Aminopterin Chemical Structure

Aminopterin Chemical Structure

CAS No. 54-62-6

Purity & Quality Control

Batch: E100301 DMSO]88 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 98.83%
98.83

Aminopterin Related Products

Signaling Pathway

DHFR Signaling Pathways

DHFR Signaling Pathway

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 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.[3]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models NOD/SCID mice
Dosages 0.5 mg/kg, 0.25 mg/kg
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00937027 Completed
Psoriasis
Syntrix Biosystems Inc.|National Institute of Allergy and Infectious Diseases (NIAID)
 June 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 440.41 Formula

C19H20N8O5
CAS No. 54-62-6 SDF --
Smiles NC1=NC(=C2N=C(CNC3=CC=C(C=C3)C(=O)NC(CCC(O)=O)C(O)=O)C=NC2=N1)N
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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