5-DACTHF
(Synonyms: 543U76; 5,11-Methenyltetrahydrohomofolate)
5-DACTHF (543U76) is an inhibitor of purine de novo biosynthesis. 5-DACTHF is a GAR-TFase and AICAR-TFase inhibitor (IC50: 3 and 94 μM). 5-DACTHF is a potent antitumor agent.
For research use only. We do not sell to patients.
- CAS No.: 118252-44-1
- Formula: C19H24N6O6
- Molecular Weight:432.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
5-DACTHF (543U76) is an inhibitor of purine de novo biosynthesis. 5-DACTHF is a GAR-TFase and AICAR-TFase inhibitor (IC50: 3 and 94 μM). 5-DACTHF is a potent antitumor agent[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-427 | IC50 |
43 nM
Compound: 1
|
Antitumor activity on A-427 lung carcinoma cell lines
Antitumor activity on A-427 lung carcinoma cell lines
|
[PMID: 2299624] |
| CCRF-CEM | IC50 |
0.198 μM
Compound: 5-DACTHF
|
Cytotoxicity against human lymphoblastic leukemic CCRF-CEM cell line was evaluated as the concentration required for 50% inhibition of the growth of the control value
Cytotoxicity against human lymphoblastic leukemic CCRF-CEM cell line was evaluated as the concentration required for 50% inhibition of the growth of the control value
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[PMID: 1552503] |
| CCRF-CEM | IC50 |
198 nM
Compound: 2
|
In vitro antitumor activity was assessed from rate of cell growth of CCRF/CEM cell line
In vitro antitumor activity was assessed from rate of cell growth of CCRF/CEM cell line
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[PMID: 8027993] |
| CCRF-CEM | IC50 |
47 nM
Compound: 1
|
Antitumor activity on CCRF-CEM T-cell acute lymphoblastic leukemia cell lines
Antitumor activity on CCRF-CEM T-cell acute lymphoblastic leukemia cell lines
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[PMID: 2299624] |
| Detroit 98 | IC50 |
0.11 μM
Compound: 1
|
Evaluated in vitro for ability to inhibit the Detroit 98 cell lines
Evaluated in vitro for ability to inhibit the Detroit 98 cell lines
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[PMID: 2299624] |
| L929 | IC50 |
0.088 μM
Compound: 1
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Evaluated in vitro for ability to inhibit the L cell lines.
Evaluated in vitro for ability to inhibit the L cell lines.
|
[PMID: 2299624] |
| MCF7 | ED50 |
0.037 μM
Compound: 5-DACTHF
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Effective dose which is required to inhibit 50% of the cell growth of MCF-7 cells in culture.
Effective dose which is required to inhibit 50% of the cell growth of MCF-7 cells in culture.
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[PMID: 1995883] |
| MCF7 | IC50 |
0.037 μM
Compound: 1
|
In vitro inhibition of growth of MCF-7 human breast adenocarcinoma using 72 hours continuous exposure
In vitro inhibition of growth of MCF-7 human breast adenocarcinoma using 72 hours continuous exposure
|
[PMID: 1573633] |
| MCF7 | IC50 |
37 nM
Compound: 1
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Antitumor activity on MCF-7 breast adenocarcinoma cell lines
Antitumor activity on MCF-7 breast adenocarcinoma cell lines
|
[PMID: 2299624] |
| MCF7 | IC50 |
37 μM
Compound: 2
|
Ability to inhibit growth of MCF-7 human breast adenocarcinoma in vitro
Ability to inhibit growth of MCF-7 human breast adenocarcinoma in vitro
|
[PMID: 8027993] |
| MOLT-4 | IC50 |
0.7 μM
Compound: 1
|
Hexaglutamyl homologue inhibition activity against the AICAR formyltransferase was determined against MOLT-4
Hexaglutamyl homologue inhibition activity against the AICAR formyltransferase was determined against MOLT-4
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[PMID: 2299624] |
| MOLT-4 | IC50 |
1.2 μM
Compound: 1
|
Compound was evaluated for inhibition of [3H]methotrexate uptake into MOLT-4 cells
Compound was evaluated for inhibition of [3H]methotrexate uptake into MOLT-4 cells
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[PMID: 1573633] |
| MOLT-4 | IC50 |
1.2 μM
Compound: 2
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Ability to inhibit [3H]methotrexate transport into MOLT-4 cells in vitro
Ability to inhibit [3H]methotrexate transport into MOLT-4 cells in vitro
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[PMID: 8027993] |
| MOLT-4 | IC50 |
58 nM
Compound: 1
|
Antitumor activity on MOLT-4 T-cell acute lymphoblastic leukemia cell lines
Antitumor activity on MOLT-4 T-cell acute lymphoblastic leukemia cell lines
|
[PMID: 2299624] |
| MOLT-4 | IC50 |
94 μM
Compound: 1
|
In vitro inhibitory activity against MOLT-4 T-cell leukemia cell AICAR transformylase
In vitro inhibitory activity against MOLT-4 T-cell leukemia cell AICAR transformylase
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[PMID: 1573633] |
| MOLT-4 | IC50 |
94 μM
Compound: 1
|
Inhibition activity against AICAR formyltransferase determined against MOLT-4
Inhibition activity against AICAR formyltransferase determined against MOLT-4
|
[PMID: 2299624] |
| MOLT-4 | IC50 |
94 μM
Compound: 5-DACTHF
|
Inhibition of 5-aminoimidazole-4-carboxamide AICAR formyltransferase in MOLT-4 cells
Inhibition of 5-aminoimidazole-4-carboxamide AICAR formyltransferase in MOLT-4 cells
|
[PMID: 1995883] |
| SW480 | IC50 |
50 nM
Compound: 1
|
Antitumor activity on SW 480 colon adenocarcinoma cell lines
Antitumor activity on SW 480 colon adenocarcinoma cell lines
|
[PMID: 2299624] |
| WiDr | IC50 |
45 nM
Compound: 1
|
Antitumor activity on WiDr colon adenocarcinoma cell lines
Antitumor activity on WiDr colon adenocarcinoma cell lines
|
[PMID: 2299624] |
| WIL2 | IC50 |
>100 μM
Compound: 5-DACTHF
|
Inhibition of dihydrofolate reductase (DHFR) in WIL2 cells
Inhibition of dihydrofolate reductase (DHFR) in WIL2 cells
|
[PMID: 1995883] |
Chemical Information
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CAS No. 118252-44-1
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Molecular Weight 432.43
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Formula C19H24N6O6
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SMILES
OC(CC[C@@H](C(O)=O)NC(C(C=C1)=CC=C1NCCCC2=C(NC(N)=NC2=O)N)=O)=O
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Synonyms
543U76; 5,11-Methenyltetrahydrohomofolate
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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.
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References
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