DSM267
DSM267 is a triazolopyrimidine inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH), with an IC50 of 38 nM, while its IC50 against human DHODH exceeds 100000 nM. DSM267 is used for the in vitro systematic screening and characterization of the resistance evolution pathways of Plasmodium falciparum to DHODH inhibitors.
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- CAS 番号: 1281861-06-0
- 分子式: C15H12F5N5
- 分子量:357.29
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Parasite アイソフォーム固有の製品をすべて表示
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L1210 | EC50 |
>50 μM
Compound: 37, DSM267
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Cytotoxicity against mouse L1210 cells
Cytotoxicity against mouse L1210 cells
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[PMID: 21696174] |
DSM267 (72 h) induces Plasmodium falciparum 3D7 A10 parasites to develop resistance in vitro via single or combined point mutations in the DHODH gene or dhodh copy number increases, resulting in DSM267 EC50 values ranging from 12.8 to >500 nM, representing 5.9- to >229-fold increases in resistance relative to wild-type parasites[1].
DSM267 (72 h) induces pre-selected Plasmodium falciparum DHODH mutant lines to exhibit resistance, with DSM267 EC50 values ranging from 31.5 to >200 nM, representing 9.1- to >57.8-fold increases in resistance relative to wild-type Dd2 or 3D7 parasites[1].
DSM267 (72 h) induces Plasmodium falciparum 3D70087/ᴺ9 parasites with the V532G DHODH mutation (selected with DSM265) to exhibit cross-resistance, with DSM267 EC50 values ranging from 317 to 495 nM, representing 69.4- to 108.3-fold increases in resistance relative to wild-type 3D70087/ᴺ9 parasites[1].
DSM267 (72 h) induces Plasmodium falciparum 3D7 A10 and 3D70087/ᴺ9 parasites with DHODH mutations (C276Y, L531F, G181C, F227Y) or dhodh copy number increases (selected with DSM265) to exhibit cross-resistance, with DSM267 EC50 values ranging from 5.99 to 5361 nM, representing 1.3- to 2459-fold increases in resistance relative to wild-type parasites[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1281861-06-0
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分子量 357.29
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分子式 C15H12F5N5
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SMILES
FC(F)(F)C1=CC=C(C=C1)NC2=CC(=NC3=NC(=NN32)C(F)(F)C)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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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]. Mandt REK, et al. In vitro selection predicts malaria parasite resistance to dihydroorotate dehydrogenase inhibitors in a mouse infection model. Sci Transl Med. 2019;11(521):eaav1636. [Content Brief]
[2]. Deng X, et al. The X-ray structure of Plasmodium falciparum dihydroorotate dehydrogenase bound to a potent and selective N-phenylbenzamide inhibitor reveals novel binding-site interactions. Acta Crystallogr F Struct Biol Commun. 2015;71(Pt 5):553-559. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)