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);Dehydrogenase |
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°C |
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 |
|
注意: |
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