AGF347
AGF347 is a potent and multi-targeted antifolate that targets serine hydroxymethyltransferase (SHMT)2 in the mitochondria and SHMT1 in the cytosol, and inhibits de novo purine biosynthesis. AGF347 induces apoptosis, inhibits mTOR signaling, decreases GSH pools, and increases ROS. AGF347 inhibits proliferation of Cisplatin (HY-17394) sensitive and resistant epithelial ovarian cancer (EOC) cells. AGF347 exhibits antitumor efficacy in SKOV3 EOC xenograft mouse models. AGF347 can be used for ovarian cancer research.
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- CAS No.: 2294820-23-6
- Formule: C22H24FN5O6
- Masse moléculaire:473.45
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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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mTOR |
Human SHMT1 |
SHMT2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.8 nM
Compound: 1
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Antitumor activity against CHO cells expressing human FR-alpha (RT16) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay
Antitumor activity against CHO cells expressing human FR-alpha (RT16) transporter assessed as inhibition of cell growth measured upto 96 hrs by Cell titer blue assay
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[PMID: 37582241] |
Chemical Information
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CAS No. 2294820-23-6
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Masse moléculaire 473.45
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Formule C22H24FN5O6
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SMILES
FC(C=C1CCCCN2C3=C(NC(N)=NC3=O)C=C2)=C(C=C1)C(N[C@H](C(O)=O)CCC(O)=O)=O
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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]. Dekhne AS, et al. Cellular Pharmacodynamics of a Novel Pyrrolo[3,2-d]pyrimidine Inhibitor Targeting Mitochondrial and Cytosolic One-Carbon Metabolism. Mol Pharmacol. 2020 Jan;97(1):9-22. [Content Brief]
[2]. Wallace-Povirk A, et al. Mitochondrial and Cytosolic One-Carbon Metabolism Is a Targetable Metabolic Vulnerability in Cisplatin-Resistant Ovarian Cancer. Mol Cancer Ther. 2024 Jun 4;23(6):809-822. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGF347 Related Classifications
HY-177092 Related Classifications
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