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  3. Aminopterin

Aminopterin  (Synonyms: 4-Aminofolic acid; APGA)

Cat. No.: HY-14518 Purity: 98.67%
Handling Instructions Technical Support

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 Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.

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Aminopterin

Aminopterin 화학구조

CAS No. : 54-62-6

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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Based on 1 Customer Validation

Other Forms of Aminopterin:

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  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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 Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia[1][2].

Cellular Effect
Cell Line Type Value Description References
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
0.001 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: 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
0.32 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]
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]
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]
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]
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
31 nM
Compound: aminopterin
Inhibition of dihydrofolate reductase in HeLa cells
Inhibition of dihydrofolate reductase in HeLa cells
[PMID: 6410066]
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]
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 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
0.002 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
0.002 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: 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: 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
0.002 μM
Compound: AMT
Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells.
Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells.
[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
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
0.003 μM
Compound: AMT
Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells.
Compound was tested for its inhibitory concentration to inhibit the growth of wild type L1210 cells.
[PMID: 3462394]
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
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
0.72 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
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 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
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
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
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 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 ( 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: 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
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: 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
분자량

440.41

화학식

C19H20N8O5

CAS No.
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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
용액&용해도
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)

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
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.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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×
Volume (start)

V1

=
Concentration (final)

C2

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V2

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
순도&문서

Purity: 98.67%

References

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.

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
100 mM 0.0227 mL 0.1135 mL 0.2271 mL 0.5677 mL
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상품명:
Aminopterin
Cat. No.:
HY-14518
수량:
MCE Japan Authorized Agent: