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 番号: 2294820-23-6
- 分子式: C22H24FN5O6
- 分子量:473.45
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
|
mTOR |
Human SHMT1 |
SHMT2 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.8 nM
Compound: 1
|
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
|
[PMID: 37582241] |
化学情報
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CAS 番号 2294820-23-6
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分子量 473.45
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分子式 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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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
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)