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.
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- CAS No.: 80576-83-6
- Formule: C22H25N7O5
- Masse moléculaire:467.48
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | IC50 |
2.6 nM
Compound: 10-EDAM
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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
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[PMID: 8035423] |
| CCRF-CEM | IC50 |
3.3 nM
Compound: 10-Deazaaminopterin (edatrexate)
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Growth inhibition of CCRF-CEM human leukemic lymphoblasts
Growth inhibition of CCRF-CEM human leukemic lymphoblasts
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[PMID: 10780919] |
| Colon 26 | IC50 |
>40 μM
Compound: 10-EDAM
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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
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[PMID: 8201595] |
| Colon 26 | IC50 |
4.8 nM
Compound: 10-EDAM
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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
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[PMID: 8201595] |
| Huh-7 | CC50 |
0.0304 μM
Compound: GNF-Pf-63
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
| KB | IC50 |
3 nM
Compound: 10-EDAM
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Inhibitory concentration of compound was tested against KB tumor growth cell line
Inhibitory concentration of compound was tested against KB tumor growth cell line
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[PMID: 8201595] |
| L1210 | IC50 |
0.65 nM
Compound: 10-Et-10-DA
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Concentration inhibiting L1210 cell growth in culture
Concentration inhibiting L1210 cell growth in culture
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[PMID: 2296020] |
| L1210 | IC50 |
1.44 nM
Compound: 10-Deazaaminopterin
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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)
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[PMID: 8340923] |
| MC-38 | IC50 |
11 nM
Compound: 10-EDAM
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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
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[PMID: 8201595] |
| P388 | IC50 |
11 nM
Compound: 10-EDAM
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Compound was tested for the inhibition of dihydrofolate reductase in P388 cells
Compound was tested for the inhibition of dihydrofolate reductase in P388 cells
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[PMID: 8201595] |
| P388 | IC50 |
4.3 nM
Compound: 10-EDAM
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Inhibitory concentration of compound was tested against P388 tumor growth cell line
Inhibitory concentration of compound was tested against P388 tumor growth cell line
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[PMID: 8201595] |
| P388 | IC50 |
44 nM
Compound: 10-EDAM
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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
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[PMID: 8201595] |
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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Masse moléculaire 467.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[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)
Edatrexate Related Classifications
HY-13617 Related Classifications
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