Cat. No.: HY-14518

Aminopterin

(Synonyms: 4-Aminofolic acid; APGA)

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Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a K_i of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.

For research use only. We do not sell to patients.

Purity: 98.67%
CAS No.: 54-62-6
Formula: C₁₉H₂₀N₈O₅
Molecular Weight:440.41

Storage:

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

Aminopterin Chemical Structure

CAS No.: 54-62-6

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	4.4 nM Compound: 1	Growth inhibition of CCRF-CEM human leukemic lymphoblasts Growth inhibition of CCRF-CEM human leukemic lymphoblasts	[PMID: 10780919]
CCRF-CEM	IC₅₀	0.001 μM Compound: 10 (AMT)	Tested for cell-growth inhibition against human leukemic lymphoblast CEM cells Tested for cell-growth inhibition against human leukemic lymphoblast CEM cells	[PMID: 2898531]
CCRF-CEM	IC₅₀	0.32 μM Compound: 10 (AMT)	Tested for cell-growth inhibition against human leukemic lymphoblast CEM/MTX cells Tested for cell-growth inhibition against human leukemic lymphoblast CEM/MTX cells	[PMID: 2898531]
CCRF-CEM	IC₅₀	0.001 μM Compound: AMT	Cell growth inhibition against CEM cell from human leukemic lymphoblasts Cell growth inhibition against CEM cell from human leukemic lymphoblasts	[PMID: 3872941]
CCRF-CEM	IC₅₀	0.32 μM Compound: AMT	Cell growth inhibition against CEM/MTX cell from human leukemic lymphoblasts Cell growth inhibition against CEM/MTX cell from human leukemic lymphoblasts	[PMID: 3872941]
CCRF-CEM	IC₅₀	3 nM Compound: AMT	Tested in vitro for inhibitory concentration against CCRF-CEM human Leukemic lymphoblast by using DHFR as primary target Tested in vitro for inhibitory concentration against CCRF-CEM human Leukemic lymphoblast by using DHFR as primary target	[PMID: 8035423]
CCRF-CEM	IC₅₀	3 μM Compound: AMT	Inhibitory activity against uptake of [3H]MTX by human leukemia cells (CCRF-CEM) Inhibitory activity against uptake of [3H]MTX by human leukemia cells (CCRF-CEM)	[PMID: 8568828]
Detroit 98	IC₅₀	0.002 μM Compound: Aminopterin	Evaluated in vitro for ability to inhibit the Detroit 98 cell lines Evaluated in vitro for ability to inhibit the Detroit 98 cell lines	[PMID: 2299624]
HeLa	IC₅₀	3.6 nM Compound: AMT	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HeLa	IC₅₀	8.3 nM Compound: AMT	Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HeLa	IC₅₀	31 nM Compound: aminopterin	Inhibition of dihydrofolate reductase in HeLa cells Inhibition of dihydrofolate reductase in HeLa cells	[PMID: 6410066]
HL-60	IC₅₀	2.5 nM Compound: AMT	Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs in absence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HL-60	IC₅₀	3 nM Compound: AMT	Cytotoxicity against human HL60 cells assessed reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay Cytotoxicity against human HL60 cells assessed reduction in cell viability incubated for 48 hrs in presence of ROS scavenger pyruvate by Alamar blue assay	[PMID: 31843461]
HuTu80	EC₅₀	4.7 nM Compound: aminopterin	Inhibition of growth (cytotoxicity) of HuTu 80 cell line in vitro Inhibition of growth (cytotoxicity) of HuTu 80 cell line in vitro	[PMID: 6410066]
KB	ED₅₀	0.003 μg/mL Compound: 2	Cytotoxicity against human KB cells Cytotoxicity against human KB cells	[PMID: 448685]
L1210	IC₅₀	0.002 μM Compound: 2	Ability to inhibit L1210 murine leukemia tumor cell growth in culture after 48 hr of its exposure. Ability to inhibit L1210 murine leukemia tumor cell growth in culture after 48 hr of its exposure.	[PMID: 1992118]
L1210	IC₅₀	0.002 μM Compound: Aminopterin	Compound was evaluated for cell growth inhibition of murine (L1210) leukemic cells Compound was evaluated for cell growth inhibition of murine (L1210) leukemic cells	[PMID: 1992122]
L1210	IC₅₀	2 nM Compound: aminopterin(AMT)	Compound was evaluated for the growth inhibition of L1210 cells. Compound was evaluated for the growth inhibition of L1210 cells.	[PMID: 1995880]
L1210	IC₅₀	0.72 nM Compound: AMT	Compound was evaluated for inhibitory effect on growth of L1210 cells at IC50 (n=4) Compound was evaluated for inhibitory effect on growth of L1210 cells at IC50 (n=4)	[PMID: 2423690]
L1210	IC₅₀	0.002 μM Compound: AMT	Compound was tested for its ability to inhibit growth of L1210 mouse leukemia cells Compound was tested for its ability to inhibit growth of L1210 mouse leukemia cells	[PMID: 2871191]
L1210	IC₅₀	0.002 μM Compound: 10 (AMT)	Tested for cell-growth inhibition against mouse leukemic L1210 cells Tested for cell-growth inhibition against mouse leukemic L1210 cells	[PMID: 2898531]
L1210	IC₅₀	0.025 μM Compound: 10 (AMT)	Tested for inhibition against purified Dihydrofolate reductase from L1210 murine leukemia cells Tested for inhibition against purified Dihydrofolate reductase from L1210 murine leukemia cells	[PMID: 2898531]
L1210	IC₅₀	0.002 μM Compound: AMT	Inhibitory activity against dihydrofolate reductase(DHFR) isolated from L1210 murine leukemia cells Inhibitory activity against dihydrofolate reductase(DHFR) isolated from L1210 murine leukemia cells	[PMID: 3351853]
L1210	IC₅₀	0.002 μM Compound: AMT	Inhibitory concentration against growth of L1210 cell line Inhibitory concentration against growth of L1210 cell line	[PMID: 3385730]
L1210	IC₅₀	0.02 μM Compound: AMT	Compound was tested for its inhibitory concentration to inhibit the enzyme Dihydro Folate Reductase (DHFR) from murine L1210 leukemia cells. Compound was tested for its inhibitory concentration to inhibit the enzyme Dihydro Folate Reductase (DHFR) from murine L1210 leukemia cells.	[PMID: 3462394]
L1210	IC₅₀	84 μM Compound: AMT	Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells and a subline (L1210 / R81). Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells and a subline (L1210 / R81).	[PMID: 3462394]
L1210	IC₅₀	0.002 μM Compound: AMT	Cell growth inhibition against mouse leukemia L1210 cells Cell growth inhibition against mouse leukemia L1210 cells	[PMID: 3872941]
L1210	IC₅₀	7.9 μM Compound: AMT	Cell growth inhibition against mouse leukemia L1210/R71 cells Cell growth inhibition against mouse leukemia L1210/R71 cells	[PMID: 3872941]
L1210	IC₅₀	84 μM Compound: AMT	Cell growth inhibition against mouse leukemia L1210/R81 cells Cell growth inhibition against mouse leukemia L1210/R81 cells	[PMID: 3872941]
L1210	IC₅₀	2.1 x 10^-9 M Compound: Aminopterin	Inhibitory concentration against the growth of L1210 murine leukemia cells in tissue culture. Inhibitory concentration against the growth of L1210 murine leukemia cells in tissue culture.	[PMID: 4009615]
L1210	EC₅₀	1.8 nM Compound: aminopterin	Inhibition of growth (cytotoxicity) of L1210 cell line in vitro Inhibition of growth (cytotoxicity) of L1210 cell line in vitro	[PMID: 6410066]
L1210	IC₅₀	0.6 x 10^-9 M Compound: Aminopterin	Inhibitory concentration of compound in growth of L-1210 cells Inhibitory concentration of compound in growth of L-1210 cells	[PMID: 6793726]
L1210	IC₅₀	1.2 nM Compound: Aminopterin	In vitro inhibition of L1210 cell growth in rodent neoplastic cells In vitro inhibition of L1210 cell growth in rodent neoplastic cells	[PMID: 7108907]
L1210 (R81)	IC₅₀	0.035 μM Compound: AMT	Compound was tested for its ability to inhibit purified dihydrofolate reductase(DHFR) from L1210/R81 cells Compound was tested for its ability to inhibit purified dihydrofolate reductase(DHFR) from L1210/R81 cells	[PMID: 2871191]
L1210 (R81)	IC₅₀	84 μM Compound: AMT	Compound was tested for its ability to inhibit growth of L1210/R81 cells Compound was tested for its ability to inhibit growth of L1210/R81 cells	[PMID: 2871191]
L1210 (R81)	IC₅₀	84 μM Compound: 10 (AMT)	Tested for cell-growth inhibition against mouse leukemic L1210/R81 cells Tested for cell-growth inhibition against mouse leukemic L1210/R81 cells	[PMID: 2898531]
L1210 (R81)	IC₅₀	84 μM Compound: AMT	Inhibitory concentration against growth of L1210/R81 cell line Inhibitory concentration against growth of L1210/R81 cell line	[PMID: 3385730]
L929	IC₅₀	0.0023 μM Compound: Aminopterin	Evaluated in vitro for ability to inhibit the L cell lines. Evaluated in vitro for ability to inhibit the L cell lines.	[PMID: 2299624]
PC-12	IC₅₀	>5 μM Compound: 1, TKO-10-1	Inhibition of nicotinic cholinergic receptor in rat PC12 cells assessed as inhibition of nicotine-stimulated [3H]-norepinephrine release after 30 mins by liquid scintillation counting analysis Inhibition of nicotinic cholinergic receptor in rat PC12 cells assessed as inhibition of nicotine-stimulated [3H]-norepinephrine release after 30 mins by liquid scintillation counting analysis	[PMID: 23916146]
SCC-25	IC₅₀	6.9 nM Compound: AMT	Tested for inhibitory concentration against human SCC25 cell line Tested for inhibitory concentration against human SCC25 cell line	[PMID: 8035423]
SCC-7	IC₅₀	4 nM Compound: AMT	Tested for inhibitory concentration against SCC-VII murine squamous carcinoma cell line Tested for inhibitory concentration against SCC-VII murine squamous carcinoma cell line	[PMID: 8035423]

In Vitro

The IC₅₀ value of Aminopterin (4-Aminofolic acid) against CCRF-CEM cells during 72 h of exposure is 4.4 nM^[2].
Aminopterin (4-Aminofolic acid) produces a marked inhibition of mitosis in low concentrations in human leukemic leukocytes^[4].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 54-62-6
Appearance Solid
Molecular Weight 440.41
Formula C₁₉H₂₀N₈O₅
Color Light yellow to yellow
SMILES

NC1=NC(N)=C2C(N=CC(CNC3=CC=C(C(N[C@@H](CCC(O)=O)C(O)=O)=O)C=C3)=N2)=N1
Synonyms

4-Aminofolic acid; APGA
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

1 M NaOH : 100 mg/mL (227.06 mM; ultrasonic and warming and heat to 60°C)

DMSO : 31.25 mg/mL (70.96 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

2.2706 mL

11.3531 mL

22.7061 mL

5 mM

0.4541 mL

2.2706 mL

4.5412 mL

10 mM

0.2271 mL

1.1353 mL

2.2706 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.

Molarity Calculator

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Portuguese - PT (644 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)

References

[1]. MEYER LM, et al. Aminopterin, a folic acid antagonist, in the treatment of leukemia. Am J Clin Pathol. 1949 Feb;19(2):119-26. [Content Brief]

[2]. Rosowsky A, et al. Synthesis and in vitro antifolate activity of rotationally restricted aminopterin and methotrexate analogues. J Med Chem. 2004 Dec 30;47(27):6958-63. [Content Brief]

[3]. Gebhardt DO, et al. The influence of aminopterin on limb regeneration in Ambystoma mexicanum. J Embryol Exp Morphol. 1966 Aug;16(1):143-58. [Content Brief]

[4]. F. W Gtmrz, et al. THE EFFECT OF 4-AMINO-PTEROYLGLUTAMIC ACID (AMINOPTERIN) ON HUMAN LEUKEMIC LEUKOCYTES IN VITRO. Blood (1950) 5 (2): 161-166.

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 M NaOH	1 mM	2.2706 mL	11.3531 mL	22.7061 mL	56.7653 mL
	5 mM	0.4541 mL	2.2706 mL	4.5412 mL	11.3531 mL
	10 mM	0.2271 mL	1.1353 mL	2.2706 mL	5.6765 mL
	15 mM	0.1514 mL	0.7569 mL	1.5137 mL	3.7844 mL
	20 mM	0.1135 mL	0.5677 mL	1.1353 mL	2.8383 mL
	25 mM	0.0908 mL	0.4541 mL	0.9082 mL	2.2706 mL
	30 mM	0.0757 mL	0.3784 mL	0.7569 mL	1.8922 mL
	40 mM	0.0568 mL	0.2838 mL	0.5677 mL	1.4191 mL
	50 mM	0.0454 mL	0.2271 mL	0.4541 mL	1.1353 mL
	60 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9461 mL
1 M NaOH	80 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7096 mL
1 M NaOH	100 mM	0.0227 mL	0.1135 mL	0.2271 mL	0.5677 mL

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Aminopterin

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Complete Stock Solution Preparation Table

Aminopterin

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Rare Diseases Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Withdrawn Drug Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Natural Product-like Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Natural Product and Natural Product-Like Compound Library

Bioactive Compound Library

Non-natural Amino Acid Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Aminopterin Related Classifications

Cat. No.: HY-14518