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- 产品描述： NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
- 靶点： IC50: 40 nM (hALDH1A1)
- 体内研究： NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts. Animal Model: 5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells) Dosage: 100µg/animal Administration: Intra-tumorally (i.t); every alternate day for 20 days Result: Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts.
- 参考文献：
1. Kulsum S et al. Cancer stem cell mediated acquired chemoresistance in head and neck cancer can be abrogated by Aldehydedehydrogenase 1 A1 inhibition. Mol Carcinog. 2016 Jul 6. 2. Yang SM, et al. Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1(ALDH1A1). J Med Chem. 2015 Aug 13;58(15):5967-5978.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.401 ml 12.004 ml 24.009 ml 5 mM 0.48 ml 2.401 ml 4.802 ml 10 mM 0.24 ml 1.2 ml 2.401 ml 50 mM 0.048 ml 0.24 ml 0.48 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
