Aminopterin (Synonyms: 4-Aminofolic acid; APGA)

Name: Aminopterin
Brand: MedChemExpress
SKU: HY-14518
Rating: 4.5 (1 reviews)

Cat. No.: HY-14518 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Aminopterin Chemical Structure

CAS No. : 54-62-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 448	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Aminopterin:

Aminopterin sodium Get quote
Aminopterin (Standard) Get quote

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]

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

Molecular Weight

440.41

Formula

C₁₉H₂₀N₈O₅

CAS No.

54-62-6

Appearance

Solid

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

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:

DMSO : 14.71 mg/mL (33.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (11.35 mM; ultrasonic and adjust pH to 8 with NaOH)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (271 KB) SDS (584 KB)

COA (247 KB) HNMR (278 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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	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
DMSO	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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Aminopterin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Aminopterin54-62-64-Aminofolic acid APGAAntifolateleukemicleukocytesfolicacidtetrahydrofolicanticancerimmunosuppressiveInhibitorinhibitorinhibit

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Aminopterin (Synonyms: 4-Aminofolic acid; APGA)

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Other Forms of Aminopterin:

Aminopterin Related Antibodies

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Aminopterin Related Antibodies

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Complete Stock Solution Preparation Table

Aminopterin Related Classifications

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