ML309
ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer.
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- CAS 番号: 1355446-05-7
- 分子式: C29H29FN4O2
- 分子量:484.56
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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
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R132H IDH1 96 nM (IC50) |
化学情報
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CAS 番号 1355446-05-7
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分子量 484.56
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分子式 C29H29FN4O2
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SMILES
O=C(N(C(C1=CC=CC=C1C)C(NC2CCCC2)=O)C3=CC=CC(F)=C3)CN4C5=CC=CC=C5N=C4
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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]. Davis M, et al. ML309: A potent inhibitor of R132H mutant IDH1 capable of reducing 2-hydroxyglutarate production in U87 MG glioblastoma cells. 2012 Apr 16 [updated 2013 May 8]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)