Edatrexate
Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck.
For research use only. We do not sell to patients.
- CAS No.: 80576-83-6
- Formula: C22H25N7O5
- Molecular Weight:467.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
2.6 nM
Compound: 10-EDAM
|
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 |
3.3 nM
Compound: 10-Deazaaminopterin (edatrexate)
|
Growth inhibition of CCRF-CEM human leukemic lymphoblasts
Growth inhibition of CCRF-CEM human leukemic lymphoblasts
|
[PMID: 10780919] |
| Colon 26 | IC50 |
>40 μM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against Colon 26 Mouse Colorectal Carcinoma on 4 hour exposure
Inhibitory concentration of compound was tested against Colon 26 Mouse Colorectal Carcinoma on 4 hour exposure
|
[PMID: 8201595] |
| Colon 26 | IC50 |
4.8 nM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against Colon 26 tumor growth cell line
Inhibitory concentration of compound was tested against Colon 26 tumor growth cell line
|
[PMID: 8201595] |
| Huh-7 | CC50 |
0.0304 μM
Compound: GNF-Pf-63
|
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
|
[PMID: 18579783] |
| KB | IC50 |
3 nM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against KB tumor growth cell line
Inhibitory concentration of compound was tested against KB tumor growth cell line
|
[PMID: 8201595] |
| L1210 | IC50 |
0.65 nM
Compound: 10-Et-10-DA
|
Concentration inhibiting L1210 cell growth in culture
Concentration inhibiting L1210 cell growth in culture
|
[PMID: 2296020] |
| L1210 | IC50 |
1.44 nM
Compound: 10-Deazaaminopterin
|
Inhibition of growth in L1210 murine leukemia cells in culture expressed as IC50 (nM)
Inhibition of growth in L1210 murine leukemia cells in culture expressed as IC50 (nM)
|
[PMID: 8340923] |
| MC-38 | IC50 |
11 nM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against Colon 38 tumor growth cell line
Inhibitory concentration of compound was tested against Colon 38 tumor growth cell line
|
[PMID: 8201595] |
| P388 | IC50 |
11 nM
Compound: 10-EDAM
|
Compound was tested for the inhibition of dihydrofolate reductase in P388 cells
Compound was tested for the inhibition of dihydrofolate reductase in P388 cells
|
[PMID: 8201595] |
| P388 | IC50 |
4.3 nM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against P388 tumor growth cell line
Inhibitory concentration of compound was tested against P388 tumor growth cell line
|
[PMID: 8201595] |
| P388 | IC50 |
44 nM
Compound: 10-EDAM
|
Inhibitory concentration of compound was tested against P388:Methotrexate resistant cells tumor growth cell line
Inhibitory concentration of compound was tested against P388:Methotrexate resistant cells tumor growth cell line
|
[PMID: 8201595] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Murine models of advanced metastatic disease (including E0771 mammary adenocarcinoma, T241 fibrosarcoma, Lewis lung carcinoma, B16 melanoma, or C38 colon carcinoma)[2]
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Dosage:0.14 g/kg and 0.21 g/kg
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Administration:Intraperitoneal injection; 0.14 g/kg twice weekly for 3 weeks and 0.21 g/kg weekly for 3 weeks; added Ca leucovorin (LCV) 16, 20, 24 h after Edatrexate treatment
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Result:Increased survival of tumor-bearing mice.
Showed markedly therapeutic effectiveness against advanced metastatic disease in high-dose regimen with delayed LCV rescue.
Chemical Information
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CAS No. 80576-83-6
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Molecular Weight 467.48
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Formula C22H25N7O5
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(C1=CC=C(C(CC2=NC3=C(N)N=C(N)N=C3N=C2)CC)C=C1)=O
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Synonyms
CGP 30694
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
[1]. Sirotnak FM, et al. Markedly improved efficacy of edatrexate compared to methotrexate in a high-dose regimen with leucovorin rescue against metastatic murine solid tumors. Cancer Res. 1993 Feb 1;53(3):587-91. [Content Brief]
[2]. Grant SC, et al. Edatrexate, an antifolate with antitumor activity: a review. Cancer Invest. 1993;11(1):36-45. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)