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製品番号: HY-13617

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Edatrexate

(別名: CGP 30694)

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 番号: 80576-83-6
分子式: C₂₂H₂₅N₇O₅
分子量:467.48

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Edatrexate 構造式

CAS 番号: 80576-83-6

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Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

生物活性

製品説明

Cellular Effect

Cell Line	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]

体内実験

Edatrexate (0.14 g/kg and 0.21 g/kg; i.p.; twice weekly×3 or weekly×3) exerts potent efficacy against advanced metastatic disease in tumor-bearing mice, better than MTX^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Murine models of advanced metastatic disease (including E0771 mammary adenocarcinoma, T241 fibrosarcoma, Lewis lung carcinoma, B16 melanoma, or C38 colon carcinoma)^[2]
Dosage:

0.14 g/kg and 0.21 g/kg
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
Result:

Increased survival of tumor-bearing mice.
Showed markedly therapeutic effectiveness against advanced metastatic disease in high-dose regimen with delayed LCV rescue.

化学情報

CAS 番号 80576-83-6
分子量 467.48
分子式 C₂₂H₂₅N₇O₅
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
別名

CGP 30694
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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