Methotrexate

Catalog No.S1210 Synonyms: NCI-C04671

Methotrexate Chemical Structure

Molecular Weight(MW): 454.44

Methotrexate (MTX), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH.

Size Price Stock Quantity  
In DMSO USD 134 In stock
USD 97 In stock
USD 197 In stock
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Cited by 8 Publications

3 Customer Reviews

  • Toxicity of MTX (3) and toxic analogues 5 a-e on a) hY1R-expressing MDA-MB-468 and b) non-hYR-expressing HEK293 cells. Cell viability was determined by resazurin assay. Bars represent the mean±SEM of at least three independent experiments performed in triplicate. Measurements were normalized by using only HBSS, pH 7, treated cells (set at 100 %) and ethanol-treated cells (set at 0 %). Statistical significances refer to only HBSS, pH 7, treated cells indicated as a dashed line.

    ChemMedChem, 2015, 10(5):804-14.. Methotrexate purchased from Selleck.

    A. Viability comparison of REH vector control, BCL6 overexpression, or BCL6 overexpression cells pre-treated with 79-6 (125μM) following exposure to three chemotherapy drugs (Ara-C [1 μM], MTX [50 μM], VCR [25 μM]). (* = p < 0.05 BCL6 OX to vector control and # = p < 0.05 BCL6 OX to BCL6 + 79-6).

    Oncotarget, 2016, 7(17):23439-53. Methotrexate purchased from Selleck.

  • Western blotting andrelative densitometric analyses of ERαexpression levels in regular (MCF-7) (a and a’) 4OH-tamoxifen resistant (Tam-Res) (b and b’) MCF-7cells treated for 24 hrs in complete medium with different doses of methotrexate (MTX) or vehicle (DMSO).

    J Cell Physiol, 2018, 233(5):3713-3722. Methotrexate purchased from Selleck.

Purity & Quality Control

Choose Selective DHFR Inhibitors

Biological Activity

Description Methotrexate (MTX), analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH.
Targets
hDHFR [4]
(Activated peripheral T cells)
24 nM
In vitro

Methotrexate (0.1-10 mM) induces apoptosis of in vitro activated T cells from human peripheral blood. Methotrexate achieves clonal deletion of activated T cells in mixed lymphocyte reactions. Methotrexate can selectively delete activated peripheral blood T cells by a CD95-independent pathway. [1] Methotrexate is taken up by cells via the reduced folate carrier and then is converted within the cells to polyglutamates. Methotrexate leads to diminished production of leukotriene B4 by neutrophils stimulated ex vivo. Methotrexate polyglutamates inhibit the enzyme aminoimidazolecarboxamidoadenosineribonucleotide (AICAR) transformylase more potently than the other enzymes involved in purine biosynthesis. Methotrexate is also known to suppress TNF activity by suppressing TNF-induced nuclear factor-κB activation in vitro, in part related to a reduction in the degradation and inactivation of an inhibitor of this factor, IκBα, and probably related to the release of adenosine. Methotrexate suppresses the production of both TNF and IFN-γ by T-cell-receptor-primed T lymphocytes from both healthy human donors and RA patients. Methotrexate treatment is associated with a significant decrease of TNF-α-positive CD4+ T cells, while the number of T cells expressing the anti-inflammatory cytokine IL-10 increased. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
P388D1 M1fYdYN6fG:2b4jpZ4l1gSCjc4PhfS=> NUW3ZlNrUUN3ME20Mlghdk1? M1H0clg3OzJ2MUO=
L cells MXfjfZRwfG:6aXPpeJkh[XO|YYm= M3;mTmlEPTB;OD6zJI5O MmfSPFY{OjRzMx?=
D54 NFrieFRkgXSxdH;4bYNqfHliYYPzZZk> MnjFTWM2OD1zNjDuUS=> MUe4OlMzPDF|
143B(TK-) M3\Ob4N6fG:2b4jpZ4l1gSCjc4PhfS=> NEjvXFFKSzVyPUiuPEBvVQ>? NYntWmd4QDZ|MkSxNy=>
U87MG MYLjfZRwfG:6aXPpeJkh[XO|YYm= NVfNTZVyUUN3ME2yNkBvVQ>? NYTDOY1iQDZ|MkSxNy=>
A549 NIrUNnBkgXSxdH;4bYNqfHliYYPzZZk> NGPVSlVKSzVyPUOxJI5O MVu4OlMzPDF|
H460 NU\mWpR3[3m2b4TvfIlkcXS7IHHzd4F6 NXv3NI5{UUN3ME25MlUhdk1? NIjIZm45PjN{NEGz
Daoy M4\sSIN6fG:2b4jpZ4l1gSCjc4PhfS=> M13jS2lEPTB;OTDuUS=> MmnBPFY{OjRzMx?=
U373MG NUPS[mxE[3m2b4TvfIlkcXS7IHHzd4F6 M2XNeGlEPTB;MUKgcm0> MXG4OlMzPDF|
Vero M{nCVYN6fG:2b4jpZ4l1gSCjc4PhfS=> Mlf0TWM2OD17LkKgcm0> MlXHPFY{OjRzMx?=
SCC25  MXfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NVLDZoVGhjFizszN NELPUI1KSzVyPUK3JI5O NYjMfpZLQTB{Mke5OS=>
NCI-H460 NFSwRotIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4W2O54yKM7:TR?= NHzNc2hKSzVyPUK4JI5O NH;IUWg6ODJ{N{m1
NCI-H23 NX\G[llKT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M1nRbJ4yKM7:TR?= MWXJR|UxRTR|IH7N M{K1TVkxOjJ5OUW=
NCI-H522 MoO5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3H4Z54yKM7:TR?= NYfvT2RJUUN3ME2yNlkhdk1? M{fHNFkxOjJ5OUW=
EKVX NFHJbolIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4ntT54yKM7:TR?= NXHaOYVUUUN3ME6xNFAxKG6P MVq5NFIzPzl3
HCT-116 M3uydGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NEXrZWV,OSEQvF2= NInVVppKSzVyPUOwJI5O Ml7UPVAzOjd7NR?=
HCT-15 NVXOenBzT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3v0ZZ4yKM7:TR?= MonGTWM2OD1|MDDuUS=> M1XyS|kxOjJ5OUW=
HT29 MnHaS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M{LLbp4yKM7:TR?= M3\wNmlEPTB;M{Kgcm0> NVnIPJNPQTB{Mke5OS=>
SW-620 M3rpOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MV\+NUDPxE1? NV7TXpU2UUN3ME2zN{BvVQ>? Mlz2PVAzOjd7NR?=
KM12 MXHHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MUT+NUDPxE1? NUKzeFFsUUN3ME20NkBvVQ>? MVm5NFIzPzl3
SF-539 NVvhZWR6T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVX+NUDPxE1? NIHJT4tKSzVyPUO1JI5O M4DzWVkxOjJ5OUW=
SF-268 NYrnNWFZT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M{X5cp4yKM7:TR?= MnvWTWM2OD13MjDuUS=> NWSxRZM2QTB{Mke5OS=>
SNB-75 MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MorCglEh|ryP MUXJR|UxRjFyMECwJI5O Ml7pPVAzOjd7NR?=
LOX IMVI M4PsbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NIjoTod,OSEQvF2= NXfLXHpXUUN3ME2yOkBvVQ>? M3n1fFkxOjJ5OUW=
UACC-62 MWLHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkDGglEh|ryP MULJR|UxRTJ6IH7N NUf5UWg{QTB{Mke5OS=>
SK-MEL-5 M{KySmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NUThfFI6hjFizszN M1ezUGlEPTB;OEegcm0> NYXYOJFSQTB{Mke5OS=>
MALME-3M NInZfohIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M1XzXZ4yKM7:TR?= MXHJR|UxRjFyMECgcm0> MX25NFIzPzl3
SK-MEL-28 NW\MZZhQT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NFvXN2t,OSEQvF2= M4LacWlEPTB-MUCwNEBvVQ>? MkX2PVAzOjd7NR?=
OVCAR-8 NGnuPVNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MXL+NUDPxE1? MlHFTWM2OD1|MTDuUS=> NYL1VHpnQTB{Mke5OS=>
OVCAR-5 NHmwb2tIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= Mm\lglEh|ryP M3fGZ2lEPTB-MUCwNEBvVQ>? M1izXlkxOjJ5OUW=
OVCAR-3 MlGwS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX[1ZmFJhjFizszN MlriTWM2OD1|OUigcm0> NVHEWZI1QTB{Mke5OS=>
786-0 NFL6TFNIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYn+NUDPxE1? Ml:5TWM2OD1|MzDuUS=> M3rDeVkxOjJ5OUW=
UO-31 MnT5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NXWzU5hihjFizszN NF3WNplKSzVyPUG5NUBvVQ>? NHe1T4Q6ODJ{N{m1
ACHN M{e0eWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NF7YVmN,OSEQvF2= NYLkcoZjUUN3ME20NEBvVQ>? MVK5NFIzPzl3
MCF7 NWLM[XVvT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MWr+NUDPxE1? MUnJR|UxRTN4IH7N MV65NFIzPzl3
MCF7-ADR MlXuS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHT2ZXh,OSEQvF2= NXf6OHNGUUN3ME23PEBvVQ>? NHrOOlg6ODJ{N{m1
PC-3 M1XiZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXPjUWtrhjFizszN NGHRWGJKSzVyPUKgcm0> M1fOT|kxOjJ5OUW=
DU-145 NETDNopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWixOm81hjFizszN MUPJR|UxRTJ|IH7N NVHMS|R3QTB{Mke5OS=>
CCRF-CEM MmO5S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M1rzcmVEPTB;MUSuOEBvVQ>? NVH1OJRzOTB7NU[yNlE>
R1 NEHSZoJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHvZWFVGSzVyPU[3OUBvVQ>? NWGwPY9lOTB7NU[yNlE>
R2(Bos) MYTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M3HnNmVEPTB;MU[wNEBvVQ>? M3rhSlExQTV4MkKx
R30dm MnT6S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4i2emVEPTB;MUSgcm0> NULkXZFEOTB7NU[yNlE>
FaDu M{XQc2dzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NWLSVnpjTUN3ME2xNU4{KG6P MorqNVA6PTZ{MkG=
A253 NEDlZVdIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M4PGdGVEPTB;MUSuOUBvVQ>? MUWxNFk2PjJ{MR?=
HT-29 MUTjfZRwfG:6aXPpeJkh[XO|YYm= NF\XWpBKSzVyPUOuOFUh|ryP NXy1TmFjOjN7Nki4NlQ>
COLO-320 DM NHPMN2NkgXSxdH;4bYNqfHliYYPzZZk> MmrITWM2OD13LkK1JO69VQ>? NV[w[nBKOjN7Nki4NlQ>
COLO 205 NXjjc4tm[3m2b4TvfIlkcXS7IHHzd4F6 M3fWVWlEPTB;Mz6yO{DPxE1? MmDjNlM6Pjh6MkS=
BGC-823 MYjjfZRwfG:6aXPpeJkh[XO|YYm= NV\3OFN3UUN3ME2wMlEyKM7:TR?= NWjyWoU{OTh3NUW1OlI>
Hela NYDTR3dQ[3m2b4TvfIlkcXS7IHHzd4F6 MoS4TWM2OD1yLkGg{txO MYqxPFU2PTV4Mh?=
Bel-7402 NHvCfpdkgXSxdH;4bYNqfHliYYPzZZk> NWf3dJN2UUN3ME24O{46KM7:TR?= M3jQS|E5PTV3NU[y

... Click to View More Cell Line Experimental Data

In vivo Methotrexate increases splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibits leukocyte accumulation in inflamed air pouches in mice. Methotrexate-mediated reduction in leukocyte accumulation is partially reversed by injection of adenosine deaminase (ADA) into the air pouch, completely reverses by a specific adenosine A2 receptor antagonist, 3,7-dimethyl-1-propargylxanthine (DMPX), but not affected by an adenosine A1 receptor antagonist, 8-cyclopentyl-dipropylxanthine in mice. [3]

Protocol

Solubility (25°C)

In vitro DMSO 90 mg/mL warmed (198.04 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* 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.

Chemical Information

Molecular Weight 454.44
Formula

C20H22N8O5

CAS No. 59-05-2
Storage powder
in solvent
Synonyms NCI-C04671

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03066466 Recruiting Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndrome Loyola University December 10 2019 Phase 3
NCT03066466 Recruiting Acute Myeloid Leukemia|Acute Lymphocytic Leukemia|Myelodysplastic Syndrome Loyola University December 10 2019 Phase 3
NCT03571321 Not yet recruiting Acute Lymphoblastic Leukemia|ALL Childhood|ALL University of Chicago|Incyte Corporation September 5 2019 Phase 1
NCT03571321 Not yet recruiting Acute Lymphoblastic Leukemia|ALL Childhood|ALL University of Chicago|Incyte Corporation September 5 2019 Phase 1
NCT03719560 Not yet recruiting Diffuse Large B Cell Lymphoma Brown University July 1 2019 Phase 2
NCT03719560 Not yet recruiting Diffuse Large B Cell Lymphoma Brown University July 1 2019 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID